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UNIVERSITATIS OULUENSIS MEDICA ACTA D D 1387 ACTA Justiina Ronkainen OULU 2016 D 1387 Justiina Ronkainen ROLE OF FTO IN THE GENE AND MICRORNA EXPRESSION OF MOUSE ADIPOSE TISSUES IN RESPONSE TO HIGH-FAT DIET UNIVERSITY OF OULU GRADUATE SCHOOL; UNIVERSITY OF OULU, FACULTY OF MEDICINE; MEDICAL RESEARCH CENTER; BIOCENTER OULU; OULU UNIVERSITY HOSPITAL

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Page 1: OULU 2016 D 1387 UNIVERSITY OF OULU P.O. Box 8000 FI-90014 ...jultika.oulu.fi/files/isbn9789526213453.pdf · ACTA UNIVERSITATIS OULUENSIS D Medica 1387 JUSTIINA RONKAINEN ROLE OF

UNIVERSITY OF OULU P .O. Box 8000 F I -90014 UNIVERSITY OF OULU FINLAND

A C T A U N I V E R S I T A T I S O U L U E N S I S

Professor Esa Hohtola

University Lecturer Santeri Palviainen

Postdoctoral research fellow Sanna Taskila

Professor Olli Vuolteenaho

University Lecturer Veli-Matti Ulvinen

Director Sinikka Eskelinen

Professor Jari Juga

University Lecturer Anu Soikkeli

Professor Olli Vuolteenaho

Publications Editor Kirsti Nurkkala

ISBN 978-952-62-1344-6 (Paperback)ISBN 978-952-62-1345-3 (PDF)ISSN 0355-3221 (Print)ISSN 1796-2234 (Online)

U N I V E R S I TAT I S O U L U E N S I S

MEDICA

ACTAD

D 1387

ACTA

Justiina Ronkainen

OULU 2016

D 1387

Justiina Ronkainen

ROLE OF FTO IN THE GENE AND MICRORNA EXPRESSION OF MOUSE ADIPOSE TISSUES IN RESPONSE TO HIGH-FAT DIET

UNIVERSITY OF OULU GRADUATE SCHOOL;UNIVERSITY OF OULU,FACULTY OF MEDICINE;MEDICAL RESEARCH CENTER;BIOCENTER OULU;OULU UNIVERSITY HOSPITAL

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A C T A U N I V E R S I T A T I S O U L U E N S I SD M e d i c a 1 3 8 7

JUSTIINA RONKAINEN

ROLE OF FTO IN THE GENE AND MICRORNA EXPRESSION OF MOUSE ADIPOSE TISSUES IN RESPONSE TO HIGH-FAT DIET

Academic dissertation to be presented with the assentof the Doctoral Training Committee of Health andBiosciences of the University of Oulu for public defencein the Leena Palotie auditorium (101A) of the Faculty ofMedicine (Aapistie 5 A), on 4 November 2016, at 12noon

UNIVERSITY OF OULU, OULU 2016

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Copyright © 2016Acta Univ. Oul. D 1387, 2016

Supervised byProfessor Markku SavolainenDoctor Tuire Salonurmi

Reviewed byDocent Eerika SavontausDocent Marjukka Kolehmainen

ISBN 978-952-62-1344-6 (Paperback)ISBN 978-952-62-1345-3 (PDF)

ISSN 0355-3221 (Printed)ISSN 1796-2234 (Online)

Cover DesignRaimo Ahonen

JUVENES PRINTTAMPERE 2016

OpponentProfessor Vesa Olkkonen

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Ronkainen, Justiina, Role of Fto in the gene and microRNA expression of mouseadipose tissues in response to high-fat diet. University of Oulu Graduate School; University of Oulu, Faculty of Medicine; MedicalResearch Center; Biocenter Oulu; Oulu University HospitalActa Univ. Oul. D 1387, 2016University of Oulu, P.O. Box 8000, FI-90014 University of Oulu, Finland

Abstract

Obesity is associated with greater risk of several diseases, such as type 2 diabetes and metabolicsyndrome. Single nucleotide polymorphisms (SNP) within the fat mass- and obesity-associatedgene FTO are robustly associated with increased body mass index (BMI) in several age and ethnicgroups. Studies with transgenic mice support a mechanistic role for FTO protein in energymetabolism. Fto-deficient mice are leaner than wild-type and overexpression of Fto leads to obesephenotype; however, the precise mechanism of FTO action in the control of BMI has remainedobscure. Fto mRNA is most abundant in the brain while high expression is present also in whiteand brown adipose tissues (WAT and BAT, respectively). WAT stores the nutritional energy andBAT dissipates it to produce heat. Furthermore, these organs participate in a complex endocrinenetwork affecting the whole body metabolism, which is more or less disrupted in obesity. In thebrowning process, white adipocytes begin to manifest brown characteristics. MicroRNAs(miRNA) are small RNA molecules, which fine-tune post-transcriptionally the expression ofgenes important in several cellular processes, including WAT and BAT differentiation andbrowning of WAT. FTO has been shown to participate in these processes as well as miRNAregulation.

The current study used a new Fto-deficient mouse model to reveal deeper insights into the roleof Fto on genes affecting WAT and BAT differentiation and function, as well as WAT browning.Furthermore, the effects of Fto on the miRNA regulation in WAT browning and BAT wereinvestigated. Our results supported a role for Fto in adipose tissue. Fto-deficient mice wereresistant to diet-induced obesity and their WAT and BAT adipocytes did not become hypertrophicsimilar to wild-type on high-fat diet. Furthermore, the expression of genes affecting adipose tissuedifferentiation and function was altered in Fto-deficient WAT and BAT, especially after high-fatdiet, and the changes may be mediated via altered miRNA expression. Fto-deficient WAT wasmore susceptible to browning, which in part contributed to the lean phenotype of these mice.Current study supported a role for Fto in whole body metabolism and adaptation of adipose tissueto changes in dietary environment.

Keywords: brown adipose tissue, FTO, gene expression, high-fat diet, microRNAexpression, white adipose tissue, white adipose tissue browning

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Ronkainen, Justiina, Fto:n vaikutus hiiren rasvakudosten geenien ja mikro-RNA:nsäätelyssä rasvaisen ruokavalion jälkeen. Oulun yliopiston tutkijakoulu; Oulun yliopisto, Lääketieteellinen tiedekunta; Medical ResearchCenter; Biocenter Oulu; Oulun yliopistollinen sairaalaActa Univ. Oul. D 1387, 2016Oulun yliopisto, PL 8000, 90014 Oulun yliopisto

Tiivistelmä

Lihavuus on toistuvasti yhdistetty useisiin liitännäissairauksiin, kuten tyypin 2 diabetekseen jametaboliseen oireyhtymään. FTO-geenissä (fat mass- and obesity-associated) esiintyvien yhdennukleotidin muutoksien (single nucleotide polymorphia, SNP) on useissa ikä- ja etnisissä ryh-missä raportoitu liittyvän korkeampaan painoindeksiin ihmisillä. Muuntogeenisillä hiirillä teh-dyt tutkimukset tukevat FTO:n mekanistista roolia energia-aineenvaihdunnassa, sillä Fto-poisto-geeniset hiiret ovat villityypin hiiriä laihempia ja sen yliekspressio johtaa ylipainoon. FTO:ntarkka rooli painon säätelyssä on kuitenkin vielä epäselvä. Fto:ta tuotetaan eniten aivoissa, muttamyös valkoisessa ja ruskeassa rasvassa. Valkoinen rasva varastoi ravinnosta saatavan energian jaruskea hajottaa sitä lämmöntuotantoon. Näillä kudoksilla on lisäksi tärkeä rooli energia-aineen-vaihdunnan monimutkaisessa verkostossa. Valkoisen rasvakudoksen ruskettumisprosessissa val-koiset rasvasolut alkavat muistuttaa ruskeita rasvasoluja. Mikro-RNA:t (miRNA) ovat pieniäRNA-juosteita, jotka hienosäätävät geenien ekspressiota transkription jälkeen ja vaikuttavatuseisiin solun tärkeisiin tapahtumiin, myös valkoisen ja ruskean rasvasolun erilaistumiseen jaruskettumiseen. FTO osallistuu näihin prosesseihin sekä miRNA-säätelyyn.

Tämän tutkimuksen tavoitteena oli selventää Fto:n roolia valkoisen ja ruskean rasvakudok-sen erilaistumisessa ja toiminnassa Fto-poistogeenisen hiirimallin avulla. Lisäksi selvitettiinFto:n vaikutuksia valkoisen rasvan ruskettumiseen ja ruskean rasvan toimintaan osallistuvienmiRNA:iden säätelyyn. Tulokset tukivat FTO:n roolia rasvakudoksessa. Fto-poistogeeniset hii-ret eivät lihoneet rasvaisella ruokavaliolla eivätkä niiden rasvasolut varastoineet rasvaa yhtä pal-jon kuin villityypin hiirillä rasvaisen ruokavalion jälkeen. Lisäksi Fto-poistogeenisen rasvaku-doksen erilaistumiseen ja toimintaan liittyvien geenien esiintyvyys muuttui erityisesti rasvaisel-la ruokavaliolla. Nämä muutokset voivat osittain selittyä muuttuneella miRNA-säätelyllä.Tulokset viittasivat siihen, että Fto-poistogeeninen valkoinen rasvakudos oli alttiimpaa ruskettu-miselle, mikä osaltaan vaikutti Fto-poistogeenisten hiirten laihuuteen. Tutkimus tuki Fto-geeninroolia energia-aineenvaihdunnan säätelyssä sekä rasvakudoksen mukautumisessa ruokavalionmuutoksiin.

Asiasanat: FTO, geeniekspressio, mikro-RNA-ekspressio, rasvainen ruokavalio, ruskearasvakudos, valkoinen rasvakudos, valkoisen rasvakudoksen ruskettuminen

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Acknowledgements

This study was conducted in the Department of Internal Medicine, Biocenter Oulu,

University of Oulu and Medical Research Center, Oulu University Hospital. I

appreciate the vision of the people who have created the facilities for science in

these institutes.

I owe my deepest gratitude to my supervisors Professor Markku Savolainen

and Doctor Tuire Salonurmi. Markku provided fantastic facilities, working

environment and encouragement during the time I spent in his group. His vast

knowledge and support was very motivating and important to me. I am especially

grateful to Tuire, who was enormous support during this project. She provided me

this fascinating topic to study and endless enthusiasm regarding experimental and

scientific questions. I want to thank the official referees Docent Eriika Savontaus

and Docent Marjukka Kolehmainen for their comments and inspiring conversations

that greatly improved this thesis. I thank MA Anna Vuolteenaho for the careful

revision of the language.

I express my gratitude to all my co-authors. Especially I am deeply indebted to

Docent Sylvain Sebért whose intelligence and vision constituted the exciting view

for the original articles and who helped with the summary figure illustrated in the

discussion of this thesis. I express my warmest gratitude to Marja-Leena

Kytökangas, Saara Korhonen and Sari Pyrhönen for the excellent technical

assistance and help in numerous problems in the field of science and life. I thank

Tuija Huusko, Antti Nissinen and Saeid Haghighi for the technical and

methodological help. I greatly acknowledge the former and current members of our

group Timo, Tiia, Anna-Maria, Sanna, Marketta, Satu and Minna for the shared

moments and ideas. The help of our secretaries Marita Ahola and Terttu Niemelä

has been invaluable during these years. I acknowledge Risto Bloigu for the help in

statistical analysis. All my former and current colleagues and friends at the CRC,

Saija, Elina, Nina, Minna, Meiju, Elina M and Heta are greatly acknowledged for

the shared coffee and lunch breaks with important conversations and their expertise

in all matters of life.

Warmest thanks go to my network of good friends. Veera, Maarit, Merja, Aino,

Annika and Satu, you have provided me enormous support and laughter during my

entire life. Special thanks to the Kuusamo hairy sisters and the beautiful Bättre Folk

posse for the best memories. I thank my parents, Tarja and Timo for giving me a

solid basis for life and supporting my decisions unconditionally. I also thank my

sister Eveliina for the help and advises in every situations, including this project. I

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thank my brother Iisakki and his fiancé Janina for the graphical expertise and good

company. I have always felt loved and safe because of my family and friends.

This work was financially supported by the Biocenter Oulu, the Sigrid Juselius

Foundation, the University of Oulu Scholarship Foundation and the Academy of

Finland.

Oulu, September 19, 2016 Justiina Ronkainen

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Abbreviations

A adenosine

Adam17 a disintegrin and metallopeptidase domain 17

ALKBH AlkB homolog

AR adiposity rebound

ATP adenosine triphosphate

Ay nonagouti mutation mouse model with human metabolic syndrome

phenotype

BAT brown adipose tissue

Bdnf brain-derived neurotrophic factor gene

BMI body mass index

C cytosine

C/EBP CCAAT/enhancer binding protein

CaMKII calcium/calmodulin-dependent protein kinase II

cAMP cyclic adenosine monophosphate

CD control diet

Cebpa C/EBPα gene

Cebpb C/EBPβ gene

Cpefat carboxypeptidase E-deficient mouse model with diabetic phenotype

CREB cAMP response element binding protein

D2R dopamine receptor type 2

D3R dopamine receptor type 3

DNA deoxyribonucleic acid

eWAT epididymal WAT

f6A N6-formyladenosine

Fto mouse fat mass- and obesity-associated gene

FTO human fat mass- and obesity-associated gene

FTO fat mass- and obesity-associated protein

Fto-KO Fto-knockout

G guanine

H adenosine, cytosine or uracil

HEK293 human embryonic kidney 293 cell

HFD high-fat diet

HH hedgehog

hm6A N6-hydroxymethyladenosine

IFNγ interferon γ

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IRX3 iroquois homeobox 3

KO knockout

Lepob leptin-deficient mouse model

Leprdp leptin receptor-deficient mouse model

LRS leucyl-tRNA synthetase

m3T 3-methylthymidine

m5C 5-methylcytosine

m6A N6-methyladenosine

MCE mitotic clonal expansion

MEF mouse embryonic fibroblast

mESC mouse embryonic stem cell

METTL3 methyltransferase-like 3

miRNA microRNA

mTORC1 mechanistic target of rapamycin complex 1

MYF5 myogenic factor 5

NPY neuropeptide Y

Npy1r neuropeptide receptor 1 gene

PCR polymerase chain reaction

PDGFRα platelet-derived growth factor α

PPAR peroxisome proliferator activated receptor

Prdm16 PR domain containing 16

PREF1 preadipocyte factor 1

R adenosine or guanine

RNA ribonucleic acid

ROCK Rho-associated protein kinase

rRNA ribosomal RNA

RT-qPCR quantitative real-time reverse-transcriptase PCR

Runx1t1 runt-related transcription factor 1 gene

scWAT subcutaneous WAT

SNP single nucleotide polymorphism

SNS sympathetic nervous system

SRPK1 SRSF protein kinase 1

SRSF2 serine/arginine-rich splicing factor 2

TGFβ transforming growth factor β

tRNA transfer RNA

tub adult onset obesity mouse model

U uracil

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UCP1 uncoupling protein 1

UTR untranslated region

WAT white adipose tissue

WTAP Wilms tumor 1 associated protein

YTHDF2 YTH-domain family member 2

α-KG α-ketoglutarate

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List of original publications

This thesis is based on the following publications, which are referred to throughout

the text by their Roman numerals:

I Ronkainen J, Huusko TJ, Soininen R, Mondini E, Cinti F, Mäkelä KA, Kovalainen M, Herzig KH, Järvelin MR, Sebért S, Savolainen MJ & Salonurmi T (2015) Fat mass- and obesity-associated gene Fto affects the dietary response in mouse white adipose tissue. Sci Rep 5:9233.

II Ronkainen J, Mondini E, Cinti F, Cinti S, Sebért S, Savolainen MJ & Salonurmi T (2016) Fto-deficiency affects the gene and microRNA expression involved in brown adipogenesis and browning of white adipose tissue in mice. Manuscript.

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Contents

Abstract

Tiivistelmä

Acknowledgements 7 Abbreviations 9 List of original publications 13 Contents 15 1 Introduction 17 2 Review of the literature 19

2.1 Genome-wide association studies ........................................................... 19 2.1.1 Original findings ........................................................................... 19 2.1.2 FTO SNPs associated with human obesity and adiposity ............. 20 2.1.3 Mechanism of association ............................................................ 22

2.2 Mechanism of FTO action ...................................................................... 23 2.2.1 Expression in mouse ..................................................................... 23 2.2.2 Transgenic mouse models ............................................................ 24 2.2.3 In vitro studies .............................................................................. 28

2.3 m6A in RNA ........................................................................................... 30 2.3.1 Biology and effects of m6A.......................................................... 30 2.3.2 Demethylation of m6A by FTO and ALKBH5 ............................. 32 2.3.3 Methyltransferases and m6A binding proteins ............................. 34

2.4 Adipose tissue ......................................................................................... 35 2.4.1 White, brown and beige adipocytes .............................................. 35 2.4.2 Adipogenesis ................................................................................ 38 2.4.3 Adipose tissue miRNA ................................................................. 43

3 Aims of the study 49 4 Materials and methods 51

4.1 Generation of Fto-KO mice (I) ............................................................... 51 4.2 Dietary treatment (I) ................................................................................ 52 4.3 Metabolic and physical performance (I) ................................................. 52 4.4 Light microscopy and immunohistochemistry (I, II) .............................. 53 4.5 Protein extraction and Western blotting (I) ............................................. 53 4.6 Total RNA and miRNA isolation and cDNA synthesis (I, II) ................. 54 4.7 Gene and miRNA expression studies (I, II) ............................................ 55 4.8 Statistics .................................................................................................. 56

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5 Results 59 5.1 Generation and characterization of Fto-KO mouse model (I) ................. 59 5.2 Morphology of white and brown adipose tissue (I, II) ............................ 61 5.3 Fto gene expression in the WT adipose tissue (I) ................................... 63 5.4 Adipokine production from eWAT (I) ..................................................... 64 5.5 Gene expression related to WAT adipogenesis and function (I) .............. 65 5.6 Gene expression related to browning of WAT and BAT

adipogenesis and metabolism (II) ........................................................... 66 5.7 Expression of miRNAs related to adipogenesis and adipose

tissue metabolism (II) .............................................................................. 68 6 Discussion 71

6.1 Weight development (I) ........................................................................... 71 6.2 Adipose tissue morphology (I, II) ........................................................... 72 6.3 Effect of HFD on Fto expression in WT mice (I, II) ............................... 73 6.4 Expression of genes related to white adipogenesis (I) ............................ 74 6.5 Browning of scWAT and BAT adipogenesis (II) ..................................... 75 6.6 Confounding factors ................................................................................ 76 6.7 Future prospects ...................................................................................... 77 6.8 Summary ................................................................................................. 78

7 Concluding remarks 79 References 81 Original publications 97

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1 Introduction

Obesity and overweight have become a world-wide epidemic in recent decades

with an increased risk of type 2 diabetes, metabolic syndrome, hypertension, heart

disease, stroke and certain forms of cancer (1). Development of obesity is

attributable to the interaction of genetic, developmental, behavioral and

environmental factors. Human BMI is highly heritable, and several independent

studies strongly associate SNPs in one gene – the FTO – with higher BMI (2-7).

SNPs within human FTO associate with BMI and adiposity; however, the

biological mechanism behind this association is not clear, since they do not directly

alter the actions of FTO or its mRNA expression (5). However, FTO mRNA

expression in WAT is associated with BMI independently from SNP genotype,

indicating a functional role for FTO in WAT (8-10). Evidently, placental FTO has

a role during intrauterine development, since FTO expression in the placenta is

associated with increased fetal weight and length, independently from SNP

genotype (11). FTO mRNA is expressed ubiquitously in mouse as well as man, with

the most abundant expression found in brain regions that control energy balance

(12, 13). In addition, Fto expression is decreased in WAT of several obesity mouse

models, supporting a role also in WAT (13, 14). Fto-deficient mice are leaner than

wild-type and Fto overexpression leads to obesity, further establishing its effect on

energy metabolism (15-20). In vitro studies indicate a role for FTO in adipocyte

differentiation (adipogenesis) and WAT browning as well as nutrient sensing (21-

24).

FTO gene encodes a non-heme iron and α-ketoglutarate-dependent

demethylase with substrate specificity towards N6-methyladenosine (m6A) in

single-stranded RNA (12, 25). This RNA modification was found already in the

1970s, but its physiological significance is only currently being resolved (26).

Evidently, m6A is a signal for mRNA processing and/or export from nucleus, while

the precise mechanism of the specificity for these processes is yet obscure

(reviewed in (27)). In addition, m6A has been found from miRNA binding sites

within mRNA, indicating a role for m6A in the fate of these small RNA molecules

21 to 23 nucleotides in length (28). MiRNAs fine-tune the expression of genes

important in several developmental processes, including adipogenesis (reviewed in

(29, 30)). During adipogenesis, mesenchymal stem cells differentiate with the

guidance of distinct transcription factors, first into preadipocytes and then into

mature adipocytes. White adipocytes store the excess energy while brown

adipocytes dissipate it for thermogenesis. BAT was previously considered absent

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in adult humans; however, growing evidence of BAT in adults has recently emerged

and its activity has been inversely associated with BMI (31-33). In the browning

process, white adipocytes begin to manifest characteristics of brown adipocytes,

thus dissipating energy instead of storing it (reviewed in (34)).

The current study aimed to assess the role of Fto in WAT and BAT as well as

the browning process of WAT. The metabolic phenotype of an Fto-deficient mouse

model was characterized and expression of genes and miRNAs related to

adipogenesis as well as adipose tissue function and homeostasis was determined.

In addition, mice were subjected to high-fat feeding so that the effects of Fto in the

“obesogenic” environment could be estimated.

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2 Review of the literature

2.1 Genome-wide association studies

2.1.1 Original findings

In 1999, the Fto gene (then named Fatso due to its large size) was found to be one

of the genes deleted in mouse fused toes (Ft) mutation (35). This mutation was

created via insertional mutagenesis into D region of chromosome 8 and resulted in

deletion of several hundred kilobases of genome (36). In addition to Fto, at least

five other genes are deleted in the Ft mutation: Fts, Ftm and iroquois homeobox

genes Irx3, Irx5 and Irx6 (reviewed in (37)). Homozygous Ft mice with craniofacial

malformation, fused toes (syndactyly), disorganization of spinal cord, and defects

in left-right axis formation, die at embryonic day 10. Heterozygous Ft mice display

syndactyly of forelimbs and thymic hyperplasia due to defects in programmed cell

death (36). Ft mice are a poor model for assessment of Fto functions since other

genes are affected as well, but it shows that this region in chromosome 8

(chromosome 16 in humans) is developmentally important (37). At the time of its

finding, Fto did not gain much attention, but once several groups in 2007 reported

an association between type 2 diabetes and SNPs in the human FTO gene, interest

began to rise (3-7). Findings were established with genome-wide association

studies (GWAS), which test the correlation between SNPs across the whole genome

and trace variation within the sample population (38). Further analysis showed that

the association was abolished after adjustment for BMI (weight per height squared

(kg/m2)), indicating that the effect exists via BMI, thus FTO was renamed fat mass-

and obesity-associated gene (37). Sequence analysis with subsequent functional

studies revealed that the FTO protein is a demethylase able to remove methyl

groups from single-stranded DNA and RNA (12, 39). Originally, 3-methylthymine

(m3T) was indicated as substrate for FTO, but in 2011, Jia et al. revealed that the

activity of FTO is actually more pronounced towards m6A which is the most

abundant modification found in mRNA (25). FTO mRNA is expressed in several

human and mouse tissues, with the highest expression found in the brain (4, 12).

The first Fto-deficient mice generated by Fischer et al. were leaner than wild-type,

supporting the phenotype seen in humans and indicating a functional role for FTO

in energy metabolism (15).

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2.1.2 FTO SNPs associated with human obesity and adiposity

The SNPs that are associated most strongly with obesity are located in the first and

second intron within the FTO gene and are in high linkage disequilibrium with each

other (4, 5). FTO SNP rs9939609 is a very intensively studied obesity-associated

SNP located in the first intron of FTO. Around 16% of the Caucasian population

are homozygous for the risk allele A of rs9939609, weigh approximately 3 kg more

and have 1.67-fold increased odds of obesity compared to individuals with the

protective TT genotype (4). Furthermore, association with BMI is absent at birth

but becomes significant during childhood. Increased adiposity has been associated

with FTO locus in several studies focusing on children (4, 5, 40), adolescents (40,

41) and adults (40, 42, 43). Closer analysis shows an interesting age-dependence

of FTO SNP association during post-natal development as AA genotype is

associated with BMI from 5.5 years of age onwards while inversely, TT genotype

shows association below 2.5 years of age (44). This indicates that variation within

the FTO gene may be associated with the timing of adiposity rebound (AR) during

childhood, which occurs at the same time with the genotypic switch (44). AR is a

phase of childhood when BMI growth curve rises rapidly between ages 5 to 7 years,

mainly due to increase in fat mass (45). Earlier AR is generally associated with

higher BMI and the risk of obesity in later life, the mean AR age being 3 years in

obese individuals compared with 6 years in reference population (46). Interestingly,

the effect of rs9939609 genotype on AR timing applies to BMI but not to height,

indicating that the effect is specific to an increase in adiposity, not to general

maturation (44).

Studies focusing on the relation of obesity risk FTO SNPs and energy or

macronutrient intake report controversial results. Several studies indicate that the

energy intake is increased in obesity risk FTO SNP carriers whereas others do not

confirm such association (reviewed in (47)). This discrepancy may result from too

small sample sizes and/or measuring errors due to underreporting of dietary intake

in individual studies. In a recent large-scale meta-analysis comprising over 177,000

adult individuals, an association with higher protein intake and obesity risk allele

of FTO SNP was found (48). However, the risk allele appears to relate to lower

energy intake when compared to non-risk allele carriers, which is speculated to

result from underreporting the dietary intake among people with higher BMI (48).

A similar study focusing on children and adolescents indicates that energy intake,

but not protein intake, is increased in risk allele carriers (49). This inconsistency

may be due to the fact that errors from self-reporting the food consumption are

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smaller in children than in adults. Interestingly, there is evidence of significant

interaction between FTO variation and protein intake on higher BMI in children

and adolescents, indicating that low protein intake may attenuate the effect of FTO

variation (49). Again, these results indicate that the effect of FTO variation on BMI

may be blunted by behavioral choices.

It is noteworthy that while FTO locus has the greatest effect on obesity, is the

most common and has the largest explained variance reported to date, its effect on

BMI variation is modest (50). Explained variance measures the contribution of

FTO SNPs to BMI variation and while being the largest known SNP associated

with human BMI, it is still only 0.34%, indicating a small effect on a person’s risk

of being obese (51). Furthermore, while genetic factors are estimated to account for

40–70% of BMI variation, only about 2.7 % of it may be explained by currently

known SNPs (52). In part, this discrepancy may result from a limited amount of

SNPs identified as yet, but there is growing evidence of gene-environment

interaction, which needs to be fully established (reviewed in (53)). For example,

SNPs have different effect on risk of obesity depending on the person’s year of

birth, so that one risk allele leads to a 0.16-unit increase in BMI of men born in

1930 compared with 0.47-unit increase among those born in 1970 (54). Thus, as

the environment has become more “obesogenic”, individuals with higher genetic

predisposition for obesity gain more weight compared with lower genetic risk

carriers. The gene-environment interaction is important also when suitable

intervention methods for weight loss are assessed. This is apparent in a study

revealing that individuals homozygous for the FTO SNP rs9939609 risk allele show

improved weight loss after low-fat, but not low-carbohydrate hypocaloric dietary

intervention, while the improvement is evident on both diets in the group of non-

risk allele carriers (55).

Lifestyle intervention studies show that obesity-associated SNPs within FTO

do not predict weight loss among obese individuals (56-61). There is evidence that

weight regain is higher in obesity risk allele carriers after lifestyle intervention (57,

58); however, this is not observed in all studies (59-61). This indicates that

behavioral factors such as adherence to weight loss recommendations may blunt

the FTO effects on weight regulation (57, 58). It is also speculated that as regular

physical activity very often reduces after lifestyle intervention, the effect of FTO

on BMI may then have been exposed, leading to increased weight regain in obesity

risk allele carriers (58). There seems to be no association between FTO SNPs and

lifestyle factors such as physical activity, supporting the notion that behavioral

strategies may overrule the genotypic effect of FTO SNPs (40, 59, 62, 63).

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2.1.3 Mechanism of association

SNPs within the FTO locus affecting BMI and adiposity are located in the intronic,

i.e. non-coding regions of the gene, which complicates the assessment of biological

effects behind the association (3-7). Functional mutations are not found within

linkage disequilibrium of obesity-associated SNPs, including exon 2 and exon-

intron junctions from obese individuals, indicating that the activity of FTO protein

is not altered due to obesity-associated SNPs. Thus, the mechanism of association

is more complex and not necessarily directly related to altered FTO function (5).

Indeed, studies focusing on the effects of obesity-associated SNPs on FTO mRNA

expression have revealed controversial results as discussed in the latter part of this

chapter. However, SNPs within the FTO locus affect mRNA expression of another

important developmental gene, IRX3 via long-range regulatory interactions (64).

In the study by Smemo et al. 11 FTO SNPs previously associated with increased

BMI were shown to associate with increased IRX3 expression, but not with FTO

expression in human brain. Thus, obesity-associated SNPs within the FTO gene

may alter the enhancer activity of other genes, such as IRX3. Indeed, the obesity-

associated regions of the FTO gene contain several cis-regulatory elements that

regulate the expression of near-by genes (64). Recently, Claussnitzer et al.

confirmed this long-range regulation of IRX3 and IRX5 expression, and reported

the first functional evidence of how FTO SNPs regulate energy metabolism (65).

Subcutaneous WAT preadipocytes isolated from obesity risk allele carriers of

rs1421085 SNP in the first intron of FTO exhibit impaired binding of ARID5B (AT-

rich interaction domain 5B). In non-risk allele carriers, ARID5B binds rs1421085

region and represses IRX3/5 expression. Without this repression in risk allele

carriers, IRX3/5 induces adipogenic lipid accumulation and represses

thermogenesis, leading to a developmental shift from browning to whitening

programs and loss of mitochondrial thermogenesis. IRX3/5 expression is increased

only in preadipocytes, not in the whole adipose tissue of risk allele carries,

indicating that the effect is specific to early differentiation and may thus affect other

tissues as well (65). These findings are further supported by the recent analysis of

public datasets focusing on functional elements, long-range chromatin–chromatin

interaction, enhancer activity and gene expression of the BMI-associated FTO

locus (66).

FTO SNPs have been reported to affect primary transcript level of FTO mRNA,

but the effect of SNPs on FTO gene expression across different ethnic and study

populations is obscure (67). The expression of FTO mRNA in visceral and

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subcutaneous adipose tissue associates with BMI irrespective of the SNP genotype

(8-10). In vitro adipocyte glycerol release and in vivo plasma glycerol level are

increased in women with the protective homozygous allele TT of rs9939609

irrespective of BMI, indicating a role for FTO in lipolysis (8). This supports a direct

role for FTO in adipose tissue and obesity, but does not explain the mechanism of

association between FTO variation and BMI. The expression of FTO mRNA in

placenta is associated with increased fetal weight and length as well as placental

weight independently from mother’s SNP genotype (11). This definitely indicates

a role for FTO in the intrauterine development but does not explain the association

between FTO SNPs and obesity seen after birth (11). Loss-of-function mutation

caused by substitution of 316th arginine to glutamine of the FTO protein was found

from nine members of a Palestinian Arab family (68). The affected individuals had

postnatal growth retardation, microcephaly, severe psychomotor delay, brain

deficits, facial dysmorphias and early lethality as the children died at 1 to 30 months

of age. While supporting the important role of FTO in the early development, such

drastic a phenotype may result from aggregated inactive FTO protein with toxic

effects rather than represent a true consequence of FTO deficiency in humans (68).

The first alternative is supported by results from Fto-deficient mouse models which

possess a milder, albeit distinct phenotype, as discussed in the next chapter.

Interestingly, a chromosomal duplication containing also duplication of the FTO

gene leads to obesity and mental retardation in humans, further supporting a direct

role in energy metabolism (69).

2.2 Mechanism of FTO action

2.2.1 Expression in mouse

Fto mRNA is expressed in several mouse tissues including brain, skeletal muscle,

pancreas, liver, heart, spleen, kidney, lung as well as WAT and BAT (12, 13).

Furthermore, Fto is expressed ubiquitously in whole mouse embryo at embryonic

day 13.5, indicating a role for FTO also in early development (13). The highest

expression in adult mouse is observed in the energy balance controlling regions of

the brain, such as arcuate (ARC), paraventricular (PVN), dorsomedial and

ventromedial nuclei of the hypothalamus (12, 13). Specifically, more FTO-positive

neurons in ARC and PVN are activated during eating termination than initiation

and FTO colocalizes with oxytocin, an important hormone participating in feeding

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inhibition, suggesting involvement in feeding inhibitory mechanisms (70). Indeed,

Fto overexpression increases oxytocin expression of hypothalamic neuronal cells

in vitro (71). Fasting reduces Fto expression in ARC, which reduction is not rescued

by leptin supplementation, indicating that Fto regulation is independent of

circulating leptin (12-14). In addition, while leptin has a role during embryonic

development, Lep deficiency does not alter the Fto expression pattern in Lepob

mouse embryos (13). Interestingly, when mice are divided into two groups based

on their tendency to eat “small” or “big”, the hypothalamic Fto expression is

increased in the group of “small eaters” compared with “big eaters” (70).

Hypothalamic Fto mRNA expression is not associated with food preference in mice,

nor is it affected by high-sucrose or lipid-supplemented diets (70).

Interestingly, the expression of Fto mRNA is reduced in WAT of several mouse

models of obesity, such as leptin- and leptin receptor-deficient Lepob and Leprdp

mice, Ay mice with nonagouti mutation representing a model for human metabolic

syndrome, Cpe-deficient Cpefat mice with diabetic phenotype and adult onset

obesity mouse model tub (13, 72). This supports a role for FTO in adipose tissue.

Furthermore, the expression of Fto is upregulated in mouse macrophages treated

with interferon γ (IFNγ) and lipopolysaccharide, indicating that FTO may mediate

the pathophysiology of obesity and inflammation (72). The expression of Fto in

WAT or BAT is not altered by fasting or glucose administration in mice, while in

liver and skeletal muscle, Fto expression is increased after fasting (73). Hepatic Fto

expression is at normal level when glucose is injected in to mice i.p. at the end of

fasting period. Thus, FTO may have a role in hepatic gluconeogenesis which is

increased (together with Fto expression) during fasting, resulting in increased

glucose output and subsequent increase in circulating glucose, which in turn

reduces hepatic gluconeogenic activity (73).

2.2.2 Transgenic mouse models

To date, at least nine transgenic mouse lines related to Fto have been generated,

eight of which are Fto-deficient (15-19) and one overexpressing (20) model,

summarized in Table 1.

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Ta

ble

1. F

to m

ou

se

mo

de

ls. M

od

ifie

d f

rom

(7

4).

Gen

otyp

e Tr

ansg

ene

cons

truct

G

row

th

reta

rdat

ion

Wei

ght

CD

/ H

FD

Ene

rgy

inta

ke

Ene

rgy

expe

nditu

re Fa

t mas

s /

Lean

mas

s

Phy

sica

l

activ

ity

Circ

ulat

ing

horm

one

(Ref

)

Glo

bal F

to-K

O

Del

etio

n of

exo

ns 2

-3

Yes

/ ↓

→1 ↑2

↓ / ↓

Adr

enal

ine ↑

Adi

pone

ctin

Lept

in ↓

(15)

Glo

bal F

to-K

O

Del

etio

n of

exo

n 3

Yes

/ →

→1 ↑2

→ / ↓

ND

IG

F-1 ↓

(16)

Glo

bal F

to-K

O

Del

etio

n of

exo

n 3

Yes

/ ND

1 →

/ ↓

ND

N

D

(17)

Glo

bal F

to-K

O

Loss

-of-f

unct

ion

mut

atio

n N

o ↓

/ ↓

→1

↑ ↓

/ →

Nor

epin

ephr

ine ↑

Dop

amin

e ↑

(18)

Adu

lt on

set g

loba

l Fto

-KO

Ta

mox

ifen-

indu

ced

dele

tion

of e

xon

3

No

↓ / N

D

→1

↑ / ↓

N

D

ND

(1

7)

Cen

tral n

ervo

us s

yste

m

spec

ific

Fto

-KO

Del

etio

n of

exo

n 3

in c

ells

expr

essi

ng n

estin

Yes

/ ND

1 ↑2

→ / ↓

ND

IG

F-1 ↓

(16)

Dop

amin

e ne

uron

spe

cific

Fto

-KO

Del

etio

n of

exo

n 3

in

dopa

min

e ne

uron

s

No

→ /

ND

1 →

/ →

ND

(1

9)

Adu

lt on

set h

ypot

hala

mic

Fto

-KO

Del

etio

n of

exo

n 3

with

vect

or-d

eriv

ed C

re

No

→ /

ND

↓1

/ →

N

D

ND

(1

7)

Glo

bal F

to o

vere

xpre

ssio

n In

serti

on o

f 1 o

r 2 a

dditi

onal

copi

es o

f Fto

No

↑ / ↑

↑1

,2

↑ / →

Le

ptin

(20)

Fto

-KO

Fto

-kno

ckou

t; C

D c

ontro

l die

t; H

FD h

igh-

fat d

iet; ↓

decr

ease

d re

lativ

e to

wild

-type

; → u

nalte

red

rela

tive

to w

ild-ty

pe; ↑

incr

ease

d re

lativ

e to

wild

-type

;

ND

not

det

erm

ined

; 1 abs

olut

e en

ergy

inta

ke; 2 e

nerg

y in

take

rela

tive

to le

an m

ass

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Mice with global germline Fto-knockout (Fto-KO) are generally smaller compared

with wild-type (WT) mice; however, the severity of phenotype differs between the

models (15-18). Fto-KO mice with the drastic phenotype are generated by targeted

deletion of the second and third (15) or only the third (16, 17) exon of the Fto gene.

These mice are born at Mendelian ratio and their body weight is unaltered at birth;

however, they begin to manifest growth retardation and more frequent postnatal

mortality compared with WT from the second postnatal day onwards (15-17).

Anatomical characteristics are unaltered while body weight and nose-anus length

are reduced in the Fto-KO mice compared with WT mice (15-17). The source of

body weight reduction differs between models as Fischer et al. show that both fat

and lean mass of Fto-KO mice are reduced (15) while Gao et al. report unaltered

fat mass and decreased lean mass (16). The most drastic effect of Fto-KO is related

to viability; approximately half of homozygous KO pups die within weeks after

birth in three of the global germline KO models, all with deletions in the genome

(15-17). The reason for the reduced viability is not clear, but it is speculated to

relate to phenotypic disadvantage of smaller body size since the mortality rate is

decreased by postponed weaning and reduction in litter size (15). Thus, the

mortality may not be due to FTO absence per se, but rather to unfavorable position

in the litter resulting from growth retardation.

Indeed, Fto-KO model with a more subtle phenotype, which is produced

without deletion of any part of the genome, lacks the postnatal growth retardation

and is as viable as WT (18). These Fto-KO mice are born the same size as WT

while their body weight begins to reduce at 12 weeks of age, which is mainly due

to reduced fat mass (18). It is yet unclear whether the phenotypic difference is

because of altered structure of the genome in deletion-induced Fto-KO or if there

is still some FTO activity left in the model without the deletion. The first option is

supported by the fact that the Fto locus contains a vast amount of regulatory

sequences inside non-coding regions of the gene and the SNPs related to human

BMI variation are all located in the introns of Fto gene indicating that the regulation

of other genes may be also affected (64-66). Evidently, lean phenotype does not

result from reduced caloric intake since the absolute energy intake of Fto-KO mice

is unaltered and in the case of some mouse models even increased when corrected

for lean or body mass (15-18). Fto-KO mice show increased plasma adiponectin,

improved glucose tolerance and reduced adipocyte size (15, 17). Mild improvement

in insulin sensitivity of Fto-KO mice is likely a consequence of increased

circulating adiponectin (15). Physical activity of Fto-KO mice is reduced or

unaltered depending on the mouse model. The reduction in physical activity may

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be due to increased sympathetic activity revealed by increased heat production and

plasma adrenaline concentration (15). Increased sympathetic activity may

contribute to Fto-KO WAT adipocytes to be more prone to browning process, which

is manifested by increased BAT marker gene expression (23).

To overcome the issue with reduced viability, adult-onset Fto-KO mice have

been produced by McMurray et al. (17). In this model, global Fto-KO is introduced

with tamoxifen-inducible ubiquitin-Cre recombinase system by treating mice with

tamoxifen at six weeks of age. The weight of these adult-onset Fto-KO mice begins

to reduce about one week after the tamoxifen treatment. Interestingly, the weight

reduction is mainly due to reduction in lean mass while the fat mass is in fact

increased due to Fto-KO. The weight difference between adult-onset Fto-KO and

control mice becomes smaller with time, being no longer significant at 26 weeks

of age due to redistribution of lean and fat mass (17). Conditional Fto-KO mouse

models have been generated to further untangle the tissue-specific roles of FTO (16,

17, 19). Central nervous system -specific Fto-KO mice resemble phenotypically

global Fto-KO mice, including increased postnatal mortality and growth

retardation indicating, that FTO functions in the brain to control growth (16).

However, hypothalamus-specific adult-onset Fto-KO mice have only a small

reduction in weight gain compared with WT, indicating additional functions for

FTO in peripheral tissues as well (17). Indeed, there are no structural alterations in

the adult hypothalamus of mice with global Fto-KO or indication of alterations

during embryonic development, which is further supported by unaltered

neuropeptide mRNA expression in the hypothalamus (15). Dopaminergic (DA)

neuron-specific as well as constitutive Fto-KO mice show altered control of DA

transmission, which is important in the regulation of learning, reward behavior,

motor functions and feeding (19). Specifically, FTO participates in dopamine

receptor type 2 and 3 (D2R and D3R) -mediated neuronal responses without

affecting D2R protein level per se. Interestingly, the weight development and

growth of these DA neuron specific Fto-KO mice are normal, supporting the notion

that FTO acts in several tissues to affect energy metabolism (19).

In addition to Fto-deficient models, mice with one and two additional copies

(that is three and four copies in total) of the Fto gene have been generated to reveal

insights into the effects of Fto overexpression on metabolic performance (20). Fto

overexpressing mice become heavier from four weeks of age onwards in a dose-

dependent manner so that the body weight of mice with four Fto copies is highest

while mice with two Fto copies (WT mice) are leanest. While fat mass is increased

in Fto overexpressing mice, body length as well as other anatomical features are

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unaltered. Interestingly, the phenotype is more prominent in transgenic females

than males, which is opposite to Fto-deficient models. The perigonadal WAT

adipocyte area is increased in Fto overexpressing females on control diet (CD) and

high-fat diet (HFD), while the difference is seen in male mice only on HFD. Lean

mass is increased in female mice on CD while there is no difference in male mice

or mice of either gender on HFD. Mice with four copies of Fto show glucose

intolerance when fed HFD which is not observed in mice with two or three copies.

Circulating leptin level is decreased in eight-week-old Fto overexpressing mice

while the difference is diminished by the age of 20 weeks (20).

2.2.3 In vitro studies

In addition to animal studies, several in vitro systems have been established to

further untangle the precise mechanisms behind FTO actions. Selection of in vitro

studies are summarized in Table 2.

Table 2. In vitro studies focusing on FTO.

Cell line Species FTO-related outcome (Ref)

Adipocytes

3T3-L1 Mouse mRNA expression is decreased during adipogenesis (21)

Downregulation impairs adipogenesis (21)

Downregulation after differentiation decreases ATP concentration (75)

Downregulation after differentiation decreases glucose uptake (75)

MEF Mouse mRNA is decreased upon essential amino acid deprivation (24)

Deficiency reduces early phase of adipogenesis (76)

Deficiency reduces growth rate and mRNA translation rate (77)

SGBS Human Downregulation after differentiation increases UCP1 expression (23)

Neurons

N46 Mouse mRNA is decreased upon essential amino acid deprivation (24)

SH-SY5Y Human Downregulation increases ATP concentration (75)

Downregulation decreases glucose uptake (75)

FTO and CaMKII induce genes regulating food intake (78)

Other

HeLa Human C/EBPα is able to bind and activate FTO promoter (22)

HEK293 Human mRNA is decreased upon essential amino acid deprivation (24)

C/EBPα is able to bind and activate FTO promoter (22)

FTO fat mass- and obesity-associated protein; ATP adenosine triphosphate; UCP1 uncoupling protein 1;

CaMKII calcium/calmodulin-dependent protein kinase II; C/EBPα CCAAT/enhancer binding protein α

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Studies with 3T3-L1 preadipocytes indicate that FTO is necessary for adipogenesis,

since Fto knockdown severely impairs the differentiation of preadipocytes into

mature adipocytes with concurrent increase in global m6A levels (21). A study

using mouse embryonic fibroblasts (MEF) indicate that FTO acts during early

phase of adipogenesis, mitotic clonal expansion, since Fto-KO reduced the

expression of short isoform of runt-related transcription factor 1 (Runx1t1) (76).

Further support for FTO’s involvement in adipogenesis comes from the notion that

CCAAT/enhancer binding protein α (C/EBPα), a key transcription factor also in

adipogenesis, is able to directly bind and activate Fto promoter in HeLa and human

embryonic kidney 293 (HEK293) cells (22). Besides the most plausible and

recently indicated substrate, m6A of RNA, FTO is also able to demethylate 5-

methylcytosine (m5C) from DNA (79). In this context, FTO may act as

transcriptional coactivator for the C/EBP family of transcription factors as

recombinant FTO demethylates m5C from C/EBP promoter in silico (79). C/EBPβ,

but not FTO, alone is able to activate C/EBP promoter to some extent, indicating

that FTO is an enhancer of the C/EBP protein family, but not essential for the

activation (79). FTO knockdown in differentiated SGBS adipocytes increases

uncoupling protein 1 (UCP1) expression with a subsequent increase in cyclic

adenosine monophosphate (cAMP)-stimulated respiration rate, supporting the role

for FTO in adipocyte browning process (23).

In hypothalamic N46 cells, MEFs and HEK293 cells, FTO is decreased when

essential amino acids are deprived while deprivation of non-essential amino acids

does not alter FTO protein levels (24). FTO does not seem to be the actual sensor

for cellular amino acids, since the decrease of its protein level occurs quite late, 6

hours after removal of amino acids. In addition, degradation of Fto mRNA occurs

faster than naturally, indicating an active degradation and transcriptional regulation

of Fto mRNA expression, not regulation mediated by amino acid availability (24).

Furthermore, FTO may have a role in determination of cellular energy status, since

Fto knockdown induces an ATP concentration decrease in differentiated 3T3-L1

mouse adipocytes and conversely, an increase in SH-SY5Y neurons, while glucose

uptake is decreased in both cell lines (75). Growth rate and mRNA translation rate

are reduced in Fto-KO MEFs, which is due to decreased mechanistic target of

rapamycin complex 1 (mTORC1) signaling (77). FTO modulates protein level of

leucyl-tRNA synthetase (LRS), which is critical in mTORC1 regulation in amino

acid deprivation, further supporting the role for FTO in cellular nutrient sensing

(77). A recent study shows that FTO interacts with calcium/calmodulin-dependent

protein kinase II (CaMKII) to modulate the cAMP response element binding

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protein (CREB) signaling pathway (78). Interaction between FTO and CaMKII

induces a prolongation of CREB phosphorylation in SH-SY5Y neurons, which

increases mRNA expression of neuropeptide receptor 1 (Npy1r) and brain-derived

neurotrophic factor (Bdnf), important regulators of food intake and energy

homeostasis (78). In addition, CREB promotes adipogenesis by activating C/EPBβ

and induces thermogenesis via UCP1 upregulation, indicating a CREB-mediated

role for FTO also in white and brown adipocytes (80, 81). Incubation of SH-SY5Y

cells with FTO containing loss-of-function mutation has an intermediate effect on

CREB phosphorylation, which indicates that the demethylase activity of FTO

contributes to the CREB activity, but does not fully explain the effects (78).

2.3 m6A in RNA

2.3.1 Biology and effects of m6A

Over 100 types of RNA modifications have been identified in all kingdoms of life,

of which the most intensively studied are related to ribosomal and transfer RNA

(rRNA and tRNA, respectively) due to their high cellular abundance, diversity and

importance in translation. However, modifications in messenger and long non-

coding RNA (mRNA and lncRNA, respectively) are also present and of growing

interest. m6A is the most abundant modification found in mRNA and lncRNA (26).

While this RNA modification was found already decades ago, its physiological

significance has only recently been resolved (82-84). RNA editing such as

adenosine-to-inosine and cytosine-to-uridine as well as 5’ capping of mRNA are

well-understood modifications due to their drastic impact on target RNA. However,

m6A is a more subtle modification and its effects are difficult to predict, since it

does not affect the base pairing or the general appearance of RNA (26). As there is

no change in base pairing, it is not possible to detect m6A by standard

hybridization- or sequencing-based methods. Furthermore, m6A is not susceptible

to chemical modification such as bisulfite treatment, which is used to detect m5C

in DNA. Lack of available detection methods is at least partly the reason why this

modification has received less attention compared with other DNA and RNA

modifications (28). Recent development of techniques that are sensitive enough has

launched a new era of m6A research and cellular pathways and effects for m6A

action on RNA have begun to be elucidated (Fig. 1).

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Fig. 1. Cellular pathways of N6-methyladenosine (m6A) in nuclear RNAs. N6-position of

adenosine in RNA is methylated by methyltransferase complex from which

methyltransferase-like (METTL) 3 and 14 and Wilms tumor 1 associated protein (WTAP)

have been identified. Demethylases such as fat mass- and obesity-associated protein

(FTO) and AlkB homolog 5 (ALKBH5) remove m6A from RNA. Readers of m6A, such as

YTH-domain family members (YTHDF) bind to methylated RNA and mediate specific

functions in nucleus and cytoplasm. Modified from (27).

Consensus sequence for m6A is RRACH (R=A/G, A=m6A and H=A/C/U) (82, 85).

High-throughput transcriptome-wide methods have been developed for m6A

mapping which use RNA immunoprecipitation with m6A antibody and subsequent

sequencing (28, 86). These studies show that while the consensus sequence is found

throughout the transcriptome, m6As are primarily located around stop codons, at

the beginning of 3’ untranslated region (3’UTR), within long internal exons, and

largely devoid from poly(A) tail (28, 86). It is yet unknown how this specificity is

achieved and whether cellular mechanisms that involve recognition of the above-

mentioned regions are involved in the specificity of m6A methylation. 3’UTR is

important region for RNA stability, subcellular localization and translation

regulation, indicating that m6A may have a role in these crucial processes. Majority

of m6As are found in mRNA while a fraction of m6As are also located in lncRNA

and within predicted miRNA binding sites of mRNA as discussed later in more

detail (28).

METTL14METTL3-

WTAP + Others?

Demethylation Export

Nucleus

Cytoplasm

Methylation

Transcription

DNA Nuclear RNA m6A-modified RNA

Co-transcriptional m6A installation?

Alternative splicing?

Me Nuclear m6A readers

Other functions?

Cytoplasmic m6A readers

Me

mRNA decay

YTHDF2

Me

Me

Me YTHDF1

mRNA translation

Me ?

mRNA storage?

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Evidently, upregulation of m6A accompanies neuronal maturation, since m6A

is present at low levels during embryogenesis of mouse brain but increases

dramatically by adulthood (28). Furthermore, decreased m6A in mouse embryonic

stem cells (mESC) results in improved self-renewal and when differentiated into

cardiomyocytes or neural cells, mESCs with decreased m6A show severe

impairment of differentiation (87). Thus, m6A may be required for mESCs to exit

the stem cell program and indeed, m6A targets include pluripotency-related

transcripts with dynamically controlled prevalence during differentiation in human

and mouse ESCs (87). Decreased m6A results in decreased cell proliferation rate

and expression of genes related to pluripotency, while developmental regulators are

increased, indicating that m6A is essential to maintain mESCs at ground state (88).

2.3.2 Demethylation of m6A by FTO and ALKBH5

FTO is the first demethylase identified to remove m6A from RNA, which revealed

that m6A actually is a dynamic, reversible RNA modification (25). Up to date, one

other m6A demethylase, AlkB homolog 5 (ALKBH5), has been identified (89).

Demethylase activity of ALKBH5 is comparable to FTO and they both require non-

heme iron (Fe(II)) and α-ketoglutarate (α-KG) to function (89). Structural and

functional studies show that demethylation activity of FTO, as well as ALKBH5,

is higher towards m6A in single-stranded than double-stranded nucleic acids (25,

89, 90). As illustrated in Fig. 2, FTO demethylates m6A through sequential

oxidation, first to N6-hydroxymethyladenosine (hm6A), then to N6-

formyladenosine (f6A) and finally to adenosine (A). Compared with other similar

intermediates, hm6A is relatively stable and hm6A as well as f6A are not

recognized by m6A binding proteins, indicating that also these intermediates may

represent a new type of RNA modification (91). Interestingly, ALKB5 does not

produce such intermediates, suggesting distinct reaction mechanisms between the

two m6A demethylases (89).

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Fig. 2. FTO and ALKBH5 remove methyl group of m6A by oxidation. FTO oxidizes m6A

to form N6-hydroxymethyladenosine (hm6A) and N6-formyladenosine (f6A), which

decompose back to adenosine (A). Modified from (92).

Fto depletion increases m6A abundance around splicing sites and enhances the

binding of serine/arginine-rich splicing factor 2 (SRSF2) to its target genes (21).

Specifically, Fto depletion inhibits exon skipping and promotes inclusion of

alternative exons in these SRSF2 targets via m6A modification. The increased

binding ability of SRSF2 to RNA with increased m6A may thus promote exon

inclusion in alternative splicing of FTO target genes. Indeed, Fto depletion results

in increased m6A levels in exons of Runx1t1 gene followed by significant increase

in SRSF1 binding, which in turn decreases the abundance of the short isoform of

Runx1t mRNA and protein. RUNX1T1 is an important transcription factor in

adipogenesis and expression of its short isoform is decreased concurrently with

FTO during adipocyte differentiation in 3T3-L1 cells, further supporting a direct

role for FTO and m6A in adipogenesis (21). ALKBH5 colocalizes with mRNA

splicing factors in nuclear speckles supporting a role in mRNA splicing (89).

However, m6A is not enriched around exon-exon junctions indicating that the effect

on splicing is unlikely through direct influence on binding of splicing factors (28).

ALKBH5 knockdown in HeLa cells results in increased levels of cytoplasmic RNA,

indicating also a role in mRNA export (89). The mechanism for this is not direct,

since ALKBH5 knockdown decreases the phosphorylation of splicing factor SRSF2

N

NN

N

N

DNA

MeH

N

NN

N

N

DNA

H

FTO FTO

N

NN

N

N

DNA

HO

H

N

NN

NDNA

A

-HCHO

-HCOOH

ALKBH5

Fe(II), KG, α O2 Fe(II), αKG, O2

Fe(II), KG, α O2

RNA methyltransferaseNH2

m6A hm6 6A

OH

A f

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mainly via subcellular relocation of the main kinase (SRSF protein kinase 1,

SRPK1) responsible for the phosphorylation. Thus, m6A may influence the fate of

mRNA by affecting cellular dynamics of the mRNA processing factors (89).

2.3.3 Methyltransferases and m6A binding proteins

Methyltransferases that add m6A to the substrate RNA form a multicomponent

complex that has not yet been fully characterized (27). The first identified

participant of this complex was methyltransferase-like 3 (METTL3), and recently,

METTL14 was also found to possess m6A methyltransferase activity (88, 93).

Recombinant METTL3/14 proteins form a tight complex with a stoichiometry of

1:1 and methylation activity is strongest when these proteins are incubated together,

indicating that they act together in the m6A methyltransferase complex (94).

METTL3/14 targets are involved in transcription, RNA splicing, chromatin

modification, programmed cell death and cell fate determination (88). Pre-mRNA

splicing regulator WTAP (Wilms tumor 1 associated protein) is able to interact with

METTL3/14 complex and also to affect m6A deposition of the cell, indicating that

WTAP may be part of the m6A methyltransferase complex as well (94).

YTH-domain family members (YTHDF) recognize and bind m6A. YTHDF1

has been identified to promote the translation and YTHDF2 to facilitate the

degradation of mRNA (95, 96). Knockdown of YTHDF1 from HeLa cells does not

affect m6A content of total mRNA, while it is increased in cytoplasmic non-

ribosome mRNA pool and decreased in translatable mRNA pool containing the

ribosomes (95). Conversely, binding of YTHDF2 to m6A destabilizes mRNA since

YTHDF2 knockdown decreases m6A in non-ribosome mRNA pool and increases it

in translatable mRNA pool (96). Overexpression of YTHDF2 leads to reduced m6A

of total mRNA, indicating that YTHDF2 itself affects also m6A levels (96). While

these two RNA-binding proteins have their distinct targets, they also share a large

set of common target mRNAs (95). YTHDF1 binds mRNA earlier than YTHDF2,

indicating that they may act together to promote translation of transcripts that are

dynamic and require temporary control (95). In addition to YTHDF1 and 2, two

other YTH-domain family members, YTHDF3 and YTHDC1, have been shown to

bind m6A (86, 97). The biological purpose of these and possible additional m6A

binding proteins is yet to be discovered.

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2.4 Adipose tissue

2.4.1 White, brown and beige adipocytes

WAT has an important role in buffering nutrient availability by storing excess

calories, preventing toxic accumulation of fat in non-adipose tissues and secreting

adipokines as a part of a dynamic endocrine system (reviewed in (34)). BAT is the

main site of non-shivering and adaptive thermogenesis, which are activated by cold

exposure and increased lipid rich dietary intake, respectively (reviewed in (98)).

Beige adipocytes have characteristics of white and brown adipocytes and are

recruited in the process of WAT browning as a response to cold or increased caloric

intake (34). BAT was previously considered absent in adult humans; however,

recently the presence of functional BAT has been discovered and its activity

associated with decreased BMI (34). The phenotype of brown adipocytes is

morphologically and functionally distinct from white adipocytes. While white

adipocytes comprise a single lipid droplet that fills about 90% of the cell volume,

brown adipocytes contain several small lipid droplets and multiple large

mitochondria packed with cristae (reviewed in (99)). Furthermore, mitochondria in

brown adipocytes contain UCP1, which uncouples oxidative phosphorylation from

ATP synthesis and results in energy dissipation via thermogenesis. Beige

adipocytes show features that are intermediate between white and brown, in that

the lipid droplet is multilocular and mitochondrial content is increased compared

with white adipocytes. Beige adipocytes may express UCP1 depending on their

differentiation stage (99).

Origins

The main source of white and brown precursors is vascular endothelium of adipose

tissue (100-102). As indicated in Fig. 3, BAT precursor cells are derived from

progenitors expressing myogenic factor 5 (MYF5+), thus sharing a common

developmental origin with skeletal myoblasts. The majority of WAT adipocytes

derive from MYF5- progenitors; however, lineage-tracing studies show that a

subset of WAT precursors may be of MYF5+ origins (103-105). The origin of beige

adipocytes is yet obscure. There is evidence suggesting that beige adipocytes arise

from trans-differentiation of white adipocytes, but also reports of differentiation

from specific precursors that are distinct from white and brown precursors

(reviewed in (106)). In addition, progenitors expressing platelet-derived growth

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factor α (PDGFRα+) have been identified to be bi-potential, thus having the ability

to differentiate into both white and beige adipocytes (106).

Fig. 3. Origins of white, beige and brown adipocytes. White and brown adipose tissue

(WAT and BAT) precursors derive from mesenchymal origins. WAT precursors may

originate from myogenic factor 5 positive and negative (MYF5+ and MYF5-) lineages

while BAT precursors derive exclusively from MYF5- lineage. In addition, WAT and BAT

adipocytes may be generated from endothelial cells and BAT adipocytes from stem cell-

like skeletal muscle satellite cells. WAT contains a mixture of uncoupling protein 1

negative (UCP1-) white adipocytes and positive (UCP1+) beige adipocytes, whereas BAT

is characterized by UCP1+ brown adipocytes. Modified from (34).

The physiological significance of MYF5+ population in WAT is yet largely elusive.

In mouse, the amount of MYF5+ progenitors in WAT is depot-specific, being at

comparable level to BAT in interscapular and retroperitoneal WAT, while being 15-

20 times lower in subcutaneous and perigonadal WAT (104). This distribution does

not correlate with mRNA expression of the BAT-markers Ucp1 and Prdm16 (PR

domain containing 16), while the WAT markers Hoxc8, Hoxc9 and Dpt are

expressed in the MYF5+ WAT cells. Thus, MYF5+ precursors may give rise to a

subset of white adipocytes in addition to brown adipocytes. β3-adrenoreceptor

stimulation induces beige adipocytes to arise from both MYF5+ and MYF5- cells

in WAT (104). Surprisingly however, when isolated from the same mouse

subcutaneous WAT depot, MYF5+ cells express lower levels of brown and beige

WAT adipocyte precursor

Endothelial precursor

Muscle satellite cell

BAT adipocyte precursor

MYF5 -

Mesenchymal precursors

White UCP1 - Beige UCP1 + Brown UCP1 +

Adipocyte precursor lineage origins

Adult origins

Mature adipocytes

MYF5 +

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adipocyte markers than MYF5- cells, indicating that MYF5- progenitors in WAT

may be more prone to browning (105).

Adipose tissues and homeostasis

In excess nutrient availability, energy is captured by WAT via glucose and lipid

uptake, lipogenesis and inhibition of lipolysis, which are regulated by insulin

(reviewed in (34)). Responses to energy deficits, such as fasting or increased energy

expenditure due to cold exposure, are regulated by the sympathetic nervous system

(SNS) (34). SNS neurons release noradrenaline from their nerve endings to transmit

signals, after which noradrenalin binds to adrenergic receptors on the target organ

(reviewed in (107)). In WAT, β-adrenergic SNS stimulation induces lipolysis in

which triglycerides are dissipated into glycerol and free fatty acids. WAT lipolysis

is regulated from the hypothalamus by neurons expressing neuropeptide Y (NPY)

and melanocortin. Insulin and leptin both inhibit NPY neurons, while they have

opposite effects on SNS output towards WAT. Insulin decreases and leptin increases

SNS activation with subsequent inhibition and induction of lipolysis in WAT,

respectively (107). SNS-mediated BAT thermogenesis and triglyceride-clearance

as well as SNS-innervation of BAT are controlled by the hypothalamus and other

brain regions (reviewed in (81)). Generally, increased SNS outflow toward BAT

results in increased triglyceride clearance and combustion to heat. Binding of

noradrenalin to β3-adrenergic receptor in BAT results in increased UCP1 synthesis

and lipolysis with increased fatty acid flux to mitochondria for combustion (81). In

addition, several SNS-independent routes for thermogenic response, such as irisin,

vitamin A derivatives, bile acids and FGF21, have been identified. This is an

intriguing field of research, specifically since anti-obesity drugs activating BAT via

global SNS activation have been associated with cardiovascular side effects. Thus,

drugs activating BAT thermogenesis independently of SNS may yield in a safer

way to induce negative energy balance and weight loss (reviewed in (108)).

Adiponectin and leptin

Adipokines, i.e., adipose tissue cytokines are secreted from adipose tissue to

modulate the metabolism and function of other distant targets such as central

nervous system, skeletal muscle, liver, cardiovascular system, and pancreas.

Numerous adipokines have been identified from which adiponectin and leptin are

introduced next in more detail. Expression of the adiponectin gene Adipoq is

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regulated by transcription factors such as peroxisome proliferator activated

receptor γ (PPARγ) and C/EBPs. Adiponectin maintains “healthy” adipose tissue

expansion, which enhances lipid storage and insulin sensitivity. Decreased plasma

adiponectin level is associated with obesity and type 2 diabetes in humans

(reviewed in (109, 110)). Circulating leptin levels are inversely correlated with fat

mass. In the hypothalamus, leptin binds to receptors that stimulate anorexigenic

peptides and in skeletal muscle, liver and pancreatic β cells, it reduces intracellular

lipid levels with subsequent improvement in insulin sensitivity. Absence of either

leptin or leptin receptor leads to severe obesity mainly due to hyperphagia

(reviewed in (111)). In addition, leptin is decreased after fasting, indicating other

regulation of its secretion aside from fat mass (109).

2.4.2 Adipogenesis

Adipocyte differentiation, i.e., adipogenesis, consists of chronological changes in

the expression of genes that eventually determine the adipocyte phenotype. It is

divided into three distinct phases: (i) lineage commitment of stem cell, (ii)

determination of committed preadipocyte and finally (iii) terminal differentiation

into mature adipocyte (Fig. 4). While WAT and BAT adipocytes derive from distinct

mesenchymal progenitors, they share a similar transcription factor cascade.

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Fig. 4. Overview of adipogenesis. Several pro- and anti-adipogenic factors participate

in maturation of mesenchymal stem cell first to preadipocyte and then to mature

adipocyte. BMP bone morphogenetic protein; Wnt wingless-type MMTV integration site;

C/EBP CCAAT/enhancer binding protein; PPARγ peroxisome proliferator activated

receptor γ. Modified from (112).

Lineage commitment

Adipocytes originate from pluripotent mesenchymal stem cells (MSCs) that have

the capability to develop into several cell lines such as adipocytes, osteoblasts,

chondrocytes, neurons and myocytes (reviewed in (113)). These stem cells can be

isolated from various human and mouse tissues. In adipose tissue, MSCs reside in

the vasculature, specifically in the endothelium (100-102). Several signaling

pathways participate in the lineage commitment of MSC to differentiate into

adipocyte. These pathways include Bone morphogenetic protein (BMP) signaling,

Wingless-type MMTV integration site (WNT) signaling, Hedgehog (HH) signaling

and NOTCH signaling (113, 114). Since lineage determination is regulated by a

network of signaling pathways and MSC may have several destinies, it is the

balance of the signaling factors that ultimately determines the lineage. In addition,

one pathway may often simultaneously promote one lineage and inhibit another

(114).

Mesenchymal stem cell Committed preadipocyte Mature adipocyte

BMP4

BMP2

Pro-adipogenic factors

Wnt5b

miR-26 miR-193b-365 miR-378

Wnt5a

Wnt10b

miR-27 miR-130 miR-155 miR-196a miR-106b-93

Extracellular matrix stiffness Increased mechanical tension Low cell confluence

Determination Terminal

differentiation

Anti-adipogenic factors

C/EBPα C/EBPδC/EBPβ PPARγ

C/EBP signaling cascade

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BMPs are members of the transforming growth factor β (TGFβ) superfamily

that have pleiotropic effects on various cells during development (115). BMP4

induces an adipogenic commitment in mouse C3H10T1/2 stem cells, a commercial

in vitro model for MSCs (115). Together with specific cofactors, BMP2 at low

concentration induces adipogenic lineage commitment whereas a high dose drives

osteogenic and chondrogenic differentiation (113, 116). Also cell shape is

implicated in stem cell fate decision. This occurs via RhoA GTPase and its effects

on Rho kinase (ROCK)-mediated cytoskeletal tension (117). Specifically, low level

of RhoA induces adipogenic differentiation of hMSC, while high level results in

osteogenic commitment even without traditional differentiation cocktails (118).

WNTs are a family of secreted glycoproteins acting in an autocrine and

paracrine manner to regulate tissue homeostasis and remodeling (119). Two distinct

routes for WNT actions are the canonical pathway that acts via β-catenin and the

non-canonical pathway that is independent of β-catenin (reviewed in (119, 120)).

The canonical WNT inhibits β-catenin phosphorylation, which stabilizes it and

results in increasing amount of cytoplasmic β-catenin that can enter into the nucleus.

In the nucleus, β-catenin dimerizes with specific transcription factors by displacing

their corepressors and subsequently regulates the transcription of target genes (120).

Disruption of β-catenin signaling induces adipogenesis while stabilization of β-

catenin induces osteogenesis (121, 122). The non-canonical WNT pathway is more

divergent and leads to regulation of intracellular activity of such enzyme as

CaMKII which, interestingly, is also associated with FTO as discussed in chapter

2.2.3 (120). Generally, the canonical WNT pathway inhibits adipogenesis by

inhibition of PPARγ and C/EBPα whereas the non-canonical pathway promotes

adipogenesis by antagonism of the canonical pathway (123-125).

Similarly to canonical WNT, HH signaling inhibits adipogenesis and promotes

osteogenesis during MSC lineage commitment (126, 127). While HH signaling is

downregulated during adipocyte differentiation, its inhibition is not sufficient to

activate adipogenesis in hMSCs (127). Interestingly, HH signaling is decreased in

human and mouse obesity, indicating that increased HH activity inhibits adipose

tissue expansion in vivo (128, 129). Furthermore, IFNγ is elevated in obesity and

opposes the HH-induced repression of adipogenesis, suggesting that HH plays a

role in adipocyte hyperplasia and pathophysiology of obesity (129). Evidently,

NOTCH signaling has a dual role in adipogenesis since both constitutive

expression and downregulation of Hes1, a target of NOTCH, reduces adipogenesis

(130). C/EBPβ is unaltered while C/EBPα and PPARγ are completely blocked due

to retroviral overexpression of Hes1 while knockdown of Hes1 induces an increase

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in preadipocyte factor 1 (PREF1), which is anti-adipogenic. PREF1 is increased in

preadipocytes and down-regulated prior to terminal differentiation being absent in

mature adipocytes, indicating that NOTCH signaling is also a prerequisite for

adipogenesis via inhibition of PREF1 (130).

Mitotic clonal expansion and determination

MSCs become preadipocytes when they lose their ability to differentiate into other

mesenchymal lineages, thus becoming ‘committed’ to the adipocytic lineage.

Several, but not all, cellular models of adipogenesis require few rounds of cell

division between lineage commitment and determination (reviewed in (131). This

event is named mitotic clonal expansion (MCE) and while it has not been

established as an unequivocal requirement for adipogenesis in all cellular models

(incl. human bone marrow MSCs), several cell cycle proteins that regulate mitosis

also regulate adipocyte differentiation supporting MCE to be a valid phase of

adipogenesis in vivo (131). C/EBPβ and δ are the main transcription factors acting

during the determination phase of adipogenesis (132). C/EBPβ/δ are distributed

diffusely into nucleus between 4 and 12 h after differentiation induction; however,

they begin to localize to centromeric satellite DNA between 12 and 24 h as the

preadipocytes enter S phase. This coincides with the phosphorylation of

retinoblastoma (RB), an important hallmark of cell cycle progression into S phase

(133). RB signaling evidently affects MCE by association with C/EBPβ, resulting

in inhibition of C/EBPβ-DNA binding (132). Phosphorylated RB is not able to

inhibit C/EBPβ, which couples the RB phosphorylation with C/EBPβ activation

subsequently driving adipogenesis onwards (132). Interestingly, while C/EBPβ/δ is

expressed rapidly after differentiation induction (within 4 h) of 3T3-L1

preadipocytes, expression of C/EBPα is induced much later, about 30 h after

differentiation is initiated (133). Furthermore, C/EBPα becomes associated with

centromeric satellite DNA between 24 and 48 h after induction of differentiation,

permitting C/EBPβ/δ to bind its promoter. Thus, C/EBPβ/δ become associated with

centromeres, possibly via RB phosphorylation, at the onset of MCE and

subsequently gain the ability to bind and activate C/EBPα promoter. C/EBPα is

anti-mitotic; the indicated time lag between C/EBPβ/δ and C/EBPα activation may

thus be crucial for MCE to be completed (133).

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Terminal differentiation

C/EBPβ and δ activate the expression of PPARγ and C/EBPα by direct binding to

their promoters to complete the differentiation of preadipocyte into mature

adipocyte (133). Furthermore, C/EBPα and PPARγ synergistically activate each

other and the adipogenic genes to achieve and maintain the mature adipocyte

phenotype (134). C/EBPα colocalizes with the majority of PPARγ binding sites and

of genes upregulated during adipogenesis, 60% are bound by both C/EBPα and

PPARγ, while 25% are bound only by C/EBPα and only 3% by PPARγ (135).

C/EBPα and PPARγ targets include genes involved in insulin sensitivity,

lipogenesis and lipolysis, such as glucose transporter 4 (Glut4), fatty acid binding

protein 4 (Fabp4), lipoprotein lipase (Lpl), 1-acylglycerol-3-phosphate O-

acyltransferase 2 (Agpat2), perilipin and secreted adipokines adiponectin and leptin

(reviewed in (136)).

C/EBPα is a transcription factor most abundantly expressed in adipose tissue,

placenta and liver (137). Homozygous Cebpa-KO mice die within 8 hours after

birth due to severe hypoglycemia resulting mainly from defects in the liver.

Adipocytes of Cebpa-KO neonates are devoid of lipid droplets; however, these

mice frequently do not suckle after birth, which makes it unclear whether the failure

to accumulate fat is due to defects in adipocytes or secondary to absence of

substrates (137, 138). To overcome the problem of reduced viability, a conditional

Cebpa-KO mouse line was established in which Cebpa gene is under albumin

promoter, thus Cebpa is expressed only in the liver (138). BAT of these conditional

Cebpa-KO mice is unaltered while WAT is almost completely absent. Interestingly,

mammary WAT is present and morphologically similar to WT, indicating that some

adipose lineages have C/EBPα dependence, whereas others do not (138). Krüppel-

like factor 3 (KLF3), together with a corepressor CtBP (C-terminal binding protein),

represses Cebpa transcription by direct binding to its promoter with subsequent

inhibition of adipogenesis (139). In addition, early B cell factors (EBF) 1 and 2

bind and activate Cebpa and Pparg promoters to induce adipogenesis (140).

Nuclear hormone receptor PPARγ is a ligand-activated transcription factor,

which in adipose tissue acts in heterodimer with retinoid X receptor α (RXRα) and

induces genes important in adipose tissue homeostasis, function and signaling.

PPARγ has two isoforms transcribed by alternative promoter usage and alternative

first exon (reviewed in (141)). PPARγ2 is more potent in adipose tissue while

PPARγ1 also has some adipogenic action. Natural ligands for PPARγ include

polyunsaturated fatty acids, long-chain monounsaturated fatty acids and phytanic

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acid (142). Synthetic ligands such as thiazolidinedione (TZD) class of anti-diabetic

drugs are widely used as PPARγ agonists to increase insulin sensitivity in type 2

diabetes via increased adipogenesis. In addition, TZD is one of the main ingredients

of the standard adipogenic cocktail in cellular studies (141). Several KLF

transcription factors regulate PPARγ; for example, KLF2 inhibits Pparg promoter

activity while KLF5 and KLF15 activate it (143-145). In addition to coregulation

with C/EBPα, PPARγ has its own coactivators (141). One of these is PPARγ

coactivator 1α (PGC1α), which has a crucial role in brown adipogenesis and

browning of white adipocytes. Interestingly, PGC1α-mediated activation of PPARγ

does not activate all PPARγ target genes. For example, PGC1α together with

PPARγ induce Ucp1, a BAT specific gene, but not fatty acid binding protein 4

(Fabp4), which is expressed in WAT and BAT (141). This tissue and gene

specificity is obtained by phosphorylation of PGC1α which only occurs in BAT

adipocytes and leads to recruitment of phosphorylated PGC1α to PPARγ binding

site on Ucp1 promoter (146).

2.4.3 Adipose tissue miRNA

MiRNAs are post-transcriptional regulators of gene expression 21 to 24 nucleotides

(nt) in length, usually affecting mRNA translation by binding (reviewed in (147)).

MiRNA may be expressed from intron of its host gene, when the expression occurs

jointly with the host mRNA, or it can have its own promoter, which enables

independent expression (148). MiRNA target sites are usually located at the 3’UTR

or coding region of mRNA. MiRNA biogenesis is illustrated in Fig. 5. Generally,

miRNAs act as repressors of mRNA translation, although miRNA-mediated up-

regulation of mRNA expression has also been reported (147). Translation activation

by miRNAs, while being less reported than repression, is prominent in specific

situations such as mouse germ cell development (149). Mechanisms for the

activation are not completely resolved, but they include increase of mRNA stability

or translation efficiency, relief of miRNA repression and direct miRNA-induced

activation (149).

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Fig. 5. Biogenesis of microRNA. (1) RNA polymerase II (Pol II) transcribes several

hundred nt-long primary miRNA (pri-miRNA) from DNA after which miRNA stem loop is

excised from pri-miRNA by ribonuclease drosha together with RNA binding protein

DGCR8. (2) This approximately 70 nt-long hairpin, now called precursor miRNA (pre-

miRNA), is exported from nucleus by exportin-5. (3) Dicer, a cytoplasmic ribonuclease,

removes the hairpin loop from pre-miRNA creating a double-stranded miRNA duplex

from which one or both strands can be incorporated into multiprotein RNA-induced

silencing complex (RISC). (4) After this, the miRNA molecule may have three destinies;

(a) perfect pairing with target site of mRNA leads to mRNA cleavage, degradation and

repression of mRNA by RISC protein argonaute (AGO), (b) partial pairing results in

mRNA deadenylation in which polyA tail is excised by CCR4-NOT complex, leaving

mRNA vulnerable to ribonuclease activity, or (c) partial pairing may cause RISC-induced

repression by blocking mRNA translation initiation, or reading in mechanisms such as

ribosome drop-off from mRNA or destabilization of mRNA binding cap protein. Modified

from (148).

Interestingly, 67% of mRNA 3’UTRs with m6A contain also one or more predicted

miRNA binding sites, indicating interactions between m6A and miRNA pathways

(28). Furthermore, m6A peaks within miRNA binding sites are more enriched near

the 3’ end of 3’UTR, which is opposite to the distribution of m6A sites in mRNA

where m6A are most abundant near the stop codons and generally decrease in

frequency along 3’UTR length. This may indicate that a spatial separation is

required for m6A to influence the function of a downstream-bound miRNA or vice

5' UTR

Pri-miRNA

Pr -miRNAe

Pr -miRNAe

miRNA duplex

Host gene

RNA polymerase II

Drosha

DGCR8

Dicer

Passenger strandLeading strand

RISC

Translational inhibition

or inhibition of mRNA cap binding protein

Deadenylation and mRNA degradation

Direct mRNA cleavage by AGO

(c) Partial binding

( ) Partial bindingb

RISC RISC

RISC

( ) Perfect bindinga

Degraded or also incorporated into RISC

Normal translation

Ribosome

RNAse

CCR4-NOT

AAAAA

AAAAAAAA

AAAAAAAAAAAAAAAAGO

AGO

AGO

AGO

mRNA

mRNA

mRNAmRNA

Nucleus

Cytoplasm

Protein

GDP-Ran

Exportin-5

AAAAAAAAAA

mRNA cap

binding protein

GW182

5' UTR

5' UTR

5' UTR

3' UTR

3' UTR

3' UTR

3' UTR

5'

3

1

2

by, for example, ribosome drop-off

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versa (28). A recent study shows mechanistic evidence for a role of m6A in miRNA

processing (150). METTL3 recognition motif GGAC, which is also part of the m6A

consensus sequence, is enriched in pri-miRNA, but not in pre-miRNA. Knockdown

of METTL3, resulting in reduced m6A levels, causes downregulation of mature

miRNA expression, while METTL3 overexpression increases mature miRNA

levels (150). Accumulation of unprocessed pre-miRNA is observed due to loss of

METTL3, indicating that m6A is necessary for pre-miRNA processing. RNA

binding protein DGCR8 binds equally methylated and unmethylated RNA,

suggesting that m6A is not a direct signal for binding of DGCR8. Messenger RNA

tends to form secondary structures such as hairpins similar to pri-miRNA, thus a

potential role of pri-miRNA m6A may be to distinguish pri-miRNA from mRNA

hairpin and facilitate the recognition of pri-miRNA structures by DGCR8 (150).

Several miRNAs have been reported to either induce or suppress adipogenesis

and adipose tissue browning (summarized in Table 3). The majority of miRNAs

involved in adipose tissue suppress their target mRNAs; however, a subset of

miRNAs enhance the translation. A selection of key miRNAs involved in WAT and

BAT adipogenesis as well as browning of WAT is introduced next (reviewed in (29,

30)).

Table 3. Selection of miRNAs involved in white and brown adipogenesis as well as

browning of white adipose tissue. Modified from (29, 30).

miRNA Target gene Effect on adipogenesis Regulator (Ref)

BAT WAT Beige

miR-26a/b Adam17*, Ucp1 ↑ ↑ ↑ Cold temperature (151)

miR-27a/b Pparg*, Prdm16, Pgc1b,

Ppara,

↓ ↓ ↓ Cold temperature (152, 153)

miR-106b-93 Ucp1, Prdm16, Ppara*?,

Pgc1a

↓ (154)

miR-130a/b Pparg* ↓ ↓ (155)

miR-155 Cebpb*, Pgc1a, Ucp1 ↓ ↓ TGFβ1 (156)

miR-193b-365 Runx1t1*, Pparg, Cebpa ↑ ↑ PRDM16, PPARα* (157)

miR-196a Runx1t1* → ↓ ↑ Cold temperature (158)

miR-378 Cebpa*?, Cebpb*?,

Runx1t1*

→1 Cold temperature (159)

* Direct binding; 1 Increased lipogenesis; Adam17 a disintegrin and metallopeptidase domain 17; Ucp1

uncoupling protein 1; Pparg peroxisome proliferator activated receptor γ; Prdm16 PR domain containing

16; Pgc1b PPARG coactivator 1 β; Ppara peroxisome proliferator activated receptor α; Pgc1b PPARG

coactivator 1 α; Cebpa CCAAT/enhancer binding protein α; Cebpb CCAAT/enhancer binding protein β;

Runx1t1 runt-related transcription factor 1; TGFβ1 transforming growth factor β 1

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Pro-adipogenic miRNAs

Members of the miR-26 family, miR-26a and b, are upregulated during early

adipogenesis of human multipotent adipose-derived stem cells (151). Inhibition of

both miR-26a and b results in inhibition of adipogenesis while overexpression leads

to accelerated adipocyte differentiation. Furthermore, miR-26 induces pathways

related to energy dissipation and shift the mitochondrial morphology towards beige

adipocyte characteristics, indicating miR-26 to be important in the browning

process. These pro-adipogenic and pro-browning effects of miR-26 are mediated

by blunting of a disintegrin and metallopeptidase domain 17 (Adam17) mRNA

translation via direct binding its 3’UTR. Adam17 knockdown induces a phenotype

similar to miR-26a/b overexpression such as increased lipid accumulation at early

differentiation stage and increased Ucp1 expression at all stages. Furthermore, BAT

of mice exposed to cold temperature exhibits increased miR-26 and Ucp1

expression while Adam17 is downregulated, indicating that the miR-26 family is

important also in BAT-induced thermogenesis (151).

Expression of the miR-193b-365 cluster is upregulated during brown

adipogenesis (160). Markers shared by both WAT and BAT such as Pparg, Cebpa,

Adipoq, Glut4 and Fabp4 are downregulated due to miR-193b-365 inhibition in

SVF cells isolated from mouse BAT as well as subcutaneous WAT (scWAT).

Similarly, BAT-specific genes are decreased upon miR-193b-365 inhibition in BAT

and scWAT preadipocytes supporting a role also in browning. Expression of miR-

193b is induced by PRDM16 via PPARα, a BAT-specific member of PPAR

transcription factors. PPARα is able to bind the miR-193b-365 promoter region and

this effect is observed only in preadipocytes, indicating that miR-193b-365 is

important during adipogenesis but not in mature adipocytes. Specifically, miR-

193b has a binding site in the 3’UTR of Runx1t1 mRNA, an inhibitor of

adipogenesis. Furthermore, several myogenic markers are increased due to miR-

193b-365-knockdown, indicating that the lineage commitment is affected. Indeed,

miR-193b-knockdown in C2C12 myoblasts represses myogenesis and induces

adipogenesis with lipid droplet containing morphology similar to adipocytes and

expression of adipocyte markers at levels comparable to cultured brown adipocytes

(157). These in vitro results have been challenged by in vivo studies using miR-

193b-365-/- mice, which develop normal BAT, thus indicating that miR-193b-365

is not a prerequisite for brown adipogenesis. The reason for this discrepancy has

not yet been resolved, but one possibility is that in vivo, other miRNAs may

compensate for the absence of miR-193b-365 (160).

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Similarly, miR-378 is upregulated during adipogenesis of 3T3-L1

preadipocytes and ST2 mesenchymal stem cells (159). Its overexpression

stimulates lipogenesis with no effect on adipogenesis or β-oxidation and leads to

increased lipid droplet size in mature adipocytes. Expression of Pparg and Glut4 is

increased due to miR-378 overexpression. Transactivation of Glut4 promoter by

C/EBPα and β is increased in miR-378 overexpressing cells, indicating that the

effects on lipid synthesis and adipocyte gene expression are mediated at least partly

through coactivation of C/EBP transcription factors. Inhibition of miR-378

decreases triacylglycerol and phospholipid synthesis in 3T3-L1-derived adipocytes

(159).

Anti-adipogenic miRNAs

MiR-130 family members miR-130a and b reduce white and brown adipogenesis

by repressing Pparg mRNA translation via direct binding to its coding and 3’UTR

regions (155). Furthermore, miR-130 is decreased (with subsequent increase in

Pparg) in the adipose tissue of obese women compared with that of non-obese.

Overexpression of miR-130 in human preadipocytes leads to decreased Pparg, Lep

and Adipoq expression. Thus, miR-130 is suggested to prevent unscheduled

differentiation, the regulation of which may be disrupted in obesity contributing at

least in part to altered adipokine production (155). MiR-155 is induced during early

adipogenesis and declines after the induction of differentiation (156). Inhibition of

miR-155 in brown preadipocytes leads to increased lipid accumulation

accompanied by increased Cebpb, Cebpa, Pparg and Fabp4 expression, indicating

that miR-155 is a repressor of adipogenesis. Furthermore, miR-155 has a negative

role also in BAT thermogenesis since its inhibition increases the expression of Ucp1

and Pgc1a. Regulation of miR-155 occurs via TGFβ1-mediated SMAD4 signaling.

Once induced by TGFβ1, miR-155 downregulates Cebpb mRNA expression via

direct interaction with its 3’UTR. Interestingly, the miR-155 promoter contains a

binding motif for C/EPBβ indicating that miR-155 may be regulated by its own

target, which is further supported by the finding that Cebpb overexpression

decreases and downregulation increases miR-155 expression in brown

preadipocytes. In scWAT, miR-155 has similar inverse effects on Ucp1 and Pgc1a

as observed in BAT indicating that miR-155 represses also the browning of WAT

(156).

Members of the miR-27 family (a and b) are downregulated during BAT, WAT

and beige adipogenesis (152, 153). Inhibition of miR-27a/b in preadipocytes

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isolated from subcutaneous and visceral WAT stromal vascular fraction (SVF) as

well as immortalized brown adipocytes leads to increased expression of BAT

markers Prdm16, Ucp1, Pparg, Ppara, Pgc1a, Adrb3, Cidea and Fabp4 suggesting

increased browning potential and adipogenesis. Overexpression leads to full

repression of Prdm16, indicating that miR-27 is a major negative regulator of

brown adipogenesis. During white adipogenesis, overexpression of miR-27b

inhibits translation of Pparg and Cebpa mRNA via direct binding to Pparg 3’UTR

(153). MiR-196a suppresses the expression of white-specific Hoxc8 during

browning of human scWAT progenitor cells with subsequent increase in brown

markers in vitro (158). Hoxc8 mRNA contains miR-196a binding site in its 3’UTR,

indicating a direct interaction. Furthermore, cold exposure and β3-adrenergic

stimulation decrease HOXC8 protein expression and increase miR-196a expression

in mouse scWAT and BAT, but to a lesser extent in epididymal WAT (eWAT), which

is known to be the WAT depot least prone to browning. However, miR-196a

expression is lower in BAT than scWAT, is not altered during SVF brown

preadipocyte differentiation and endogenous Hoxc8 is not detected in BAT. Thus,

miR-196a may regulate beige but not brown adipogenesis (158). Cluster of miR-

106b and miR-93 also possess anti-adipogenic function since inhibition of miR-

106b-93 in brown preadipocytes leads to increased BAT marker and Adipoq

expression. Sequence analysis indicates that Ppara is a potential target for direct

miR-106b-93 binding; however, this has not yet been functionally verified (154).

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3 Aims of the study

The overall aim of this study was to reveal new insights into the role of FTO in

adipose tissue. The specific aims were:

1. To characterize the metabolic phenotype of a new Fto-deficient mouse model

2. To assess the role of Fto and high-fat diet in gene expression related to white

and brown adipogenesis and function as well as the browning process of white

adipose tissue

3. To determine the role of Fto in microRNA expression in the above-mentioned

processes.

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4 Materials and methods

4.1 Generation of Fto-KO mice (I)

The KO-construct targeting the second intron of the Fto gene is illustrated in Fig.

6. The Fto-KO mice used in the experiments, contain the whole KO-cassette in

their genome which, due to polyadenylation signal, causes termination of Fto gene

transcription inside the second intron without deleting any part of the gene.

Fig. 6. Fto-knockout construct targeting the second intron of mouse Fto gene

disrupting the transcription and leading to production of truncated mRNA. Arrows are

primer binding sites used in genotyping; E1-E9 exons 1-9; En2SA En2 splice acceptor;

β-geo fusion of β galactosidase and neomycin resistance genes; pA polyadenylation

signal; UTR untranslated region; Frt flippase recognition target site; loxP locus of

crossover in P1 site.

To generate an Fto-KO mouse line, C57BL/6N embryonic stem (ES) cells targeted

with the KO-construct were obtained from the European Conditional Mouse

Mutagenesis Program (EUCOMM). ES cells (clone EPD0103_5_G10) were

injected in blastocyst injections to C57BL/6JOlaHsd females in the transgenic core

facility of Biocenter Oulu. Transgenic mice were backcrossed to the

C57BL/6JOlaHsd background for up to three generations in the Laboratory Animal

Center, University of Oulu. WT controls were C57BL/6JOlaHsd mice and all the

experiments were conducted on male mice. The animal experiments were approved

by the University of Oulu Animal Ethics Committee and the Southern Finland

Regional State Administrative Agency (license numbers ESLH-2008-06715/Ym-

23 and ESAVI/4464/04.10.03/ 2011) and followed national Finnish legislation, the

European Convention for the protection of vertebrate animals used for

experimental and other scientific purposes (ETS 123) and EU Directive

2010/63/EU.

E2E1

E1

E4Targeted allele

Mutant transcript

Wild-type transcript

En2 SA β-geo pAFrt Frt loxP loxP

E3 E5 E6 E7 E8 E9 UTR

Neo FtoFto Neo

En2 SA β-geo pAE2

E3E1 E4 E8 E9E7E6E5E2

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Genotype was confirmed using primers specific for Fto and Neo (Table 4).

Polymerase chain reaction (PCR) protocol for Fto primers was: 95°C for 12 min,

30 cycles of (denaturation at 94°C for 30 sec, annealing at 50°C for 30 sec,

extension at 72°C for 45 sec), 72°C for 10 min, 10 °C for 1 min and 4°C forever.

Neo PCR was the same as Fto except that the annealing temperature was 55°C and

the number of cycles 32.

Table 4. Primer sequences for genotyping the transgenic mice. Primers were purchased

from Sigma-Aldrich (St. Louis, MO, USA) and the sequences are indicated from 5’ to 3’

end.

Gene Forward primer 5’ – 3’ Reverse primer 5’ – 3’

Fto TTACTGCATTCTCTTCCAGAGAGG ACGCCCAGACACTCTCCAGTGAGC

Neo TGTCATCTCACCTTGCTCCTG TCAAGAAGGCGATAGAAGGCG

4.2 Dietary treatment (I)

Male mice were housed in the Laboratory Animal Center, University of Oulu at

21±2°C temperature on 12/12-hour dark-light cycle with ad libitum access to water

and either CD or HFD. At six weeks of age, mice were allocated into four groups

according to genotype and diet: WT on CD (n=9), Fto-KO on CD (n=5), WT on

HFD (n=9) and Fto-KO on HFD (n=8). CD contained 10 kJ-% fat, 20 kJ-% protein

and 70 kJ-% carbohydrate (total energy 16.1 kJ/g) and HFD consisted 45 kJ-% fat,

20 kJ-% protein and 35 kJ-% carbohydrate (total energy 19.8 kJ/g) (D12450B and

D12451, Research Diets, New Brunswick, NJ, USA). The dietary treatment lasted

16 weeks during which the mice were weighed every two weeks and eventually

sacrificed by carbon dioxide inhalation and cervical dislocation. Specimens of

eWAT, scWAT from inguinal region and interscapular BAT were snap-frozen in

liquid nitrogen and stored at -70°C until subsequent protein and RNA isolations.

4.3 Metabolic and physical performance (I)

At the end of the 16-week dietary experiment, metabolic performance, physical

activity as well as water and food intake were analyzed in a home cage-based

monitoring system for laboratory animals (LabMaster TSE System, Bad Homburg,

Germany) as described previously in (161). Briefly, mice were housed in separate

cages and after one week of acclimatization, each of the following parameters was

measured every 30 minutes during a total period of 95 hours: water and food

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consumption were measured by sensors attached to cage lids, O2 consumption, CO2

production, respiratory exchange ratio and heat production were determined by

indirect calorimetric system and physical activity including ambulatory and fine

movement was detected by infrared light-beam sensors around the cages.

4.4 Light microscopy and immunohistochemistry (I, II)

Adipose tissue depots (eWAT, scWAT and BAT) were fixed by immersion in 4%

paraformaldehyde in 0.1M phosphate buffer pH 7.4, overnight at +4°C. After

fixation, samples were dehydrated in ethanol, cleared in xylene and embedded in

paraffin. Serial sections with thickness of 3µm were obtained from each adipose

tissue depot specimens. One section was reserved for hematoxylin and eosin

staining to assess morphology and the others for immunohistochemical processing

to determine UCP1 protein expression in scWAT and BAT.

For immunohistochemistry, sections were incubated with rabbit polyclonal

anti-UCP1 (Abcam, Cambridge, UK) diluted by 1:1000 for scWAT and 1:200 for

BAT. To inactivate endogenous peroxidase, 0.3% hydrogen peroxide was used,

followed by normal goat serum to reduce nonspecific staining. Sections were

incubated in anti-UCP1 overnight at 4°C. Biotinylated HRP-conjugated goat anti-

rabbit IgG (Vector Laboratories, Burlingame, CA) was used as secondary antibody.

Histochemical reactions were performed using Vector's Vectastain ABC Kit

(Burlingame, CA) and Sigma Fast 3,3’-diaminobenzidine as substrate (Sigma, St.

Louis, MO), and sections were counterstained with hematoxylin. Sections were

imaged with Nikon Eclipse E800 light microscope using 40X objective and images

were captured with Nikon DXM 1200 digital camera. UCP1 expression was studied

in two mice in scWAT of WT in the HFD group and in three mice in all the

remaining groups.

4.5 Protein extraction and Western blotting (I)

To ascertain that FTO was absent at protein level, proteins from eWAT, scWAT and

BAT were extracted. Protein levels of adiponectin and leptin were studied from

eWAT only. The protocol proceeded as follows, 2.5 volumes of lysis buffer (20 mM

Tris-HCl pH 7.5, 150 mM NaCl, 1% Triton-X, 2 mM EDTA, 10X Protease

Inhibitor Cocktail (Sigma-Aldrich, St-Louis, MO, USA)) were added to 100 mg of

frozen tissue and homogenized with Tissue-Lyser LT (Qiagen, Hilden, Germany)

at +4°C for 2 min at 35 Hz, then centrifuged at +4°C for 10 min at 18000 x G.

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Equal amounts of proteins were loaded to 4/20% SDS-PAGE gel and blotted to

nitrocellulose (FTO) or polyvinylidene fluoride (adiponectin and leptin)

membranes. The primary antibody for FTO was mouse anti-FTO (AG-20A-0088,

AdipoGen International, San Diego, CA, USA). Adiponectin antibody (PA1-054)

was obtained from Affinity Bioreagents (Golden, USA) and leptin antibody (500-

P68) from PeproTech (Rocky Hill, NJ, USA). Glyceraldehyde-3-phosphate

dehydrogenase (GAPDH, sc-25778, Santa Cruz Biotechnology, Dallas, TX, USA)

was used as loading control. The secondary antibody for FTO was donkey anti-rat

IgG (NBP1-73749, Novus Biologicals, Littleton, CO, USA) and for adiponectin,

leptin and GAPDH, donkey anti-rabbit IgG (NA934, GE Healthcare, UK).

Immunocomplexes were detected from the membranes using Pierce ECL Western

Blotting Substrate (Thermo Scientific, Rockford, IL, USA). Adiponectin and leptin

levels relative to the protein amount loaded to the gel were calculated from band

intensities using Fiji image analysis software (162).

4.6 Total RNA and miRNA isolation and cDNA synthesis (I, II)

Total RNA was isolated from 50-100 mg of frozen eWAT, scWAT and BAT

specimens. Tissues were homogenized using Tissue Lyser LT and QIAzol Lysis

Reagent according to manufacturer’s instructions (Qiagen, Hilden, Germany).

Total RNA and miRNA-enriched fraction were isolated separately from eWAT and

scWAT with RNeasy Mini kit and RNeasy MinElute Cleanup Kit. From BAT,

miRNA-included total RNA was isolated with miRNeasy Mini Kit (Qiagen, Hilden,

Germany). The quality and the concentration of total RNA were analyzed using

NanoDrop ND-1000 UV-Vis Spectrophotometer (NanoDrop Technologies,

Wilmington, DE, USA). Due to the small size of miRNAs, it was not possible to

measure the concentration of miRNA-enriched fraction with spectrophotometric

techniques, so fluorescence-based RediPlate 96 RiboGreen RNA Quantitation Kit

was used according to manufacturer’s instructions (Molecular Probes, Eugene, OR,

USA).

Genomic DNA was removed from total RNA with DNAase treatment after

which cDNA was synthetized from 500 ng of RNA using RevertAidTM First Strand

cDNA Synthesis Kit (Fermentas, Sankt Leon-Rot, Germany). MiRNA cDNA

synthesis was conducted from 100 ng of eWAT and scWAT miRNA-enriched

fraction and from 500 ng of BAT total RNA with qScript microRNA cDNA

Synthesis Kit (Quanta BioSciences, Gaithersburg, MD, USA).

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4.7 Gene and miRNA expression studies (I, II)

Relative expression of genes and miRNAs related to WAT and BAT adipogenesis

as well as metabolism of adipose tissue and browning of scWAT was studied by

quantitative real-time reverse-transcriptase PCR (RT-qPCR) using the ΔΔCt

method (163). β-actin (Actb) and Gapdh were used as reference genes for gene

expression analysis whereas non-coding RNAs SNORD47 and SNORD85 were

used as internal references for miRNA expression studies. The primer sequences

and annealing temperatures for the gene expression studies are shown in Table 5

and for miRNA analysis in Table 6. The primers for the gene expression studies

were purchased from Sigma-Aldrich (St. Louis, MO, USA) and for miRNA studies

from Quanta BioSciences (Gaithersburg, MD, USA).

RT-qPCR reactions of gene expression studies were performed using iCycler

thermal cycler and iQ5 Real-Time Detection System with iQ SYBR Green

Supermix (Bio-Rad Laboratories, Hercules, CA, USA). The PCR protocol was:

95°C for 3 min, 40 cycles of (95°C for 10 sec, annealing temperature for 10 sec,

72°C for 10 sec) and then 72°C for 2 min. Melting curve analysis was included at

the end of every run with increasing temperature from 55°C to 95°C at 0.5°C

intervals, 10 sec at each temperature. MiRNA expression was studied with CFX96

Real-Time PCR Detection System (Bio-Rad Laboratories, Hercules, CA, USA) and

PerfeCTa SYBR Green SuperMix (Quanta BioSciences, Gaithersburg, MD, USA).

The PCR protocol for miRNAs was: 95°C for 2 min, 40 cycles of (95°C for 5 sec,

annealing temperature for 30 sec), after which melt curve was produced with

increasing temperature from 65°C to 95°C at 0.5°C intervals, 5 sec at each

temperature. Each sample was analyzed in duplicates with inter-run calibrator and

no-template control in every plate.

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Table 5. Sequences and annealing temperatures of primers used in the RT-qPCR

studies. Primers were purchased from Sigma-Aldrich (St. Louis, MO, USA) and

sequences are indicated from 5’ to 3’ end.

Gene Forward primer 5’ – 3’ Reverse primer 5’ – 3’ Annealing °C

Actb TGGATCGGTGGCTCCATCCTGG CGCAGCTCAGTAACAGTCCGCCTA Several

Adrb3 CTCTAGTTCCCAGCGGAGTT CATAGCCATCAAACCTGTTG 62

Bmp4 AGCCGAGCCAACACTGTGAG GAGCTCTGCCGAGGAGATCAC 62

Cebpa ACGGCGGGAACGCAACAACA GCTTGCGCAGGCGGTCATTG 62

Cebpb CGCAACCTGGAGACGCAGCA GGCTCGGGCAGCTGCTTGAA 61

Fto GCGGAGGAACGAGAGCGGGA GCTGCCGGCCTCTCGGAAAA 61

Gapdh CCAATGTGTCCGTCGTGGATCT GTTGAAGTCGCAGGAGACAACC Several

Glut4 GAGCTGGTGTGGTCAATACG GTTCCAGCAGCAGCAGAG 60

Pgc1a ACAACAATGAGCCTGCGAAC GCTCCATCTGTCAGTGCATC 61

Pparg ACTCCCTCATGGCCATTGAG TGAGACATCCCCACAGCAAG 61

Prdm16 AACTGTGTCAAGGTGTTCAC GCATATGAATGGCTTCAC 59

Rxra CACCTGCCGAGACAACAAG GTTCTCATTCCGGTCCTTGC 60

Ucp1 TGCCTCACTCAGGATTGG GCTTGCATTCTGACCTTCAC 63

Table 6. Quanta BioSciences miRNA assay (Gaithersburg, MD, USA) information of

primers used in the miRNA expression studies.

miRNA Quanta BioSciences miRNA assay (ref#) Annealing °C

miR-26a hsa-miR-26a-5p (68676137) 60

mir-27a hsa-miR-27a* (68676138) 65

mir-93 HSMIR-0093 (69002641) 60

mir-130b MMIR-0130B* (69002636) 60

mir-155 MMIR-0155 (69002637) 60

mir-193b HSMIR-0193B-5P (69002642) 60

mir-365a HSMIR-0365A-5P (69002640) 60

mir-378a HSMIR-0378* (69002632) 60

mir-455 HSMIR-0455-5P (69002644) 60

SNORD47 MM-SNORD47 (69002634) 60

SNORD85 MM-SNORD85 (69002633) 60

4.8 Statistics

Variable distributions were tested with Shapiro-Wilk test and variance equalities

with Levene’s test. Logarithmic transformation was applied for skewed distribution

and/or unequal variance. Weight development was analyzed with repeated

measures ANOVA, and since there was a significant interaction effect (Wilks’

Lambda p<0.001), also with two-way ANOVA and simple main effect analysis with

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Bonferroni correction at individual time points. Phenotypic characteristics, protein

expressions as well as relative expression of genes and miRNAs were analyzed

with two-way ANOVA followed by simple main effect analysis with Bonferroni

correction if there was a significant interaction effect or possible moderation effect.

Since Fto expression was absent in Fto-KO specimens, the difference between

relative expression of Fto in WT mice after CD and HFD was analyzed with

Student’s t-test. P values lower than 0.05 were considered statistically significant

and results are expressed as mean and SEM. All analyses were conducted with IBM

SPSS Statistics software package version 20.0 (IBM, Armonk, NY, USA).

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5 Results

5.1 Generation and characterization of Fto-KO mouse model (I)

The correct targeting of the knockout cassette was verified by PCR and the

depletion of FTO protein by Western blotting (Fig. 7). Genotypes of the pups

obtained from heterozygote matings were born in the normal Mendelian ratios.

Fig. 7. Genotyping of WT and Fto-KO mice by PCR. A 500-bp fragment was produced

from WT allele with Fto primers, which lack in the Fto-KO allele. Primers targeting the

neomycin resistance gene (Neo) produced a 475-bp fragment from the Fto-KO construct,

which was not present in WT allele. (b) Absence of FTO protein in Fto-KO mice was

confirmed with Western blot. Antibody against mouse FTO and donkey anti-rat IgG as

secondary antibody were used. Recombinant FTO (Rec.FTO) was used as a positive

control (60 kDa) which was run in the same 4/20% SDS-PAGE gel and blotted to

nitrocellulose membrane under the same experimental conditions as the samples.

Dotted lines indicate the cropping lines.

The weight of the animals did not differ in the beginning of the dietary experiment;

however, from the age of eight weeks onwards, the WT mice on HFD gained more

weight in comparison to other groups (Fig. 8).

1000 bp900 bp800 bp700 bp600 bp

500 bp

400 bp

Fto NeoWT Fto-KO Rec.

FTO WT Fto-KOFto Neo

(a) (b)

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Fig. 8. Weight development of mice during 16 weeks of dietary experiment. WT wild-

type; Fto-KO Fto-knockout; CD control diet; HFD high-fat diet. Results are shown as

mean ± SEM (n=5–9 per group). Two-way ANOVA followed by simple main effects

analysis with Bonferroni correction because of the significant interaction effect in

repeated measures two-way ANOVA, **p < 0.01, ***p < 0.001 between WT and HFD

groups, except 1 between WT groups and 2 between HFD groups.

6 8 10 12 14 16 18 20 22

20

25

30

35

40

45

50

∗∗∗∗∗∗

∗∗∗

∗∗∗∗∗∗

∗∗∗∗∗∗1

∗∗2W

eig

ht

(g)

Age (wk)

WT CD

Fto-KO CD

WT HFD

Fto-KO HFD

∗∗1

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Interestingly, despite a significant difference in weight of the WT and Fto-KO mice

on HFD, no genotypic-dependent differences were observed in water or food intake

or any other measures of energy expenditure (Table 7).

Table 7. Phenotype of mice after 16 weeks’ consumption of control or high-fat diet.

p value

Parameter

Diet

WT

Fto-KO

Effect of

Genotype

Effect of

Diet

Genotype

x diet

Final weight CD 31.5 ± 1.09a 28.2 ± 1.06 < 0.001 < 0.001 0.001

(g) HFD 45.4 ± 1.07 32.3 ± 1.64a

Water intake CD 3.74 ± 0.34 3.03 ± 0.26 0.35 < 0.001 0.14

(ml) HFD 2.28 ± 0.26 2.45 ± 0.22

Energy intake CD 62.7 ± 2.8 67.0 ± 5.3 0.33 0.77 0.82

(kJ) HFD 59.6 ± 7.9 66.7 ± 3.8

Heat production CD 95.3 ± 2.1 96.3 ± 1.7 0.79 0.12 0.99

(kJ/h) HFD 100.8 ± 3.7 101.7 ± 3.7

Heat production per weight CD 3.30 ± 0.11 3.56 ± 0.22 0.40 < 0.001 0.36

(kJ/h/g) HFD 2.64 ± 0.15 2.63 ± 0.11

Respiratory exchange ratio CD 45.1 ± 0.71 45.1 ± 1.03 0.53 < 0.001 0.48

(VCO2/VO2) HFD 37.9 ± 0.62 38.8 ± 0.37

Ambulatory movement CD 8429 ± 1577 10098 ± 1190 0.79 0.01 0.24

(counts) HFD 6596 ± 593 5527 ± 951

Fine movement CD 6546 ± 1169 7829 ± 774 0.66 0.09 0.30

(counts) HFD 5927 ± 400 5395 ± 790

Total movement CD 17480 ± 1312 17927 ± 1948 0.90 < 0.001 0.81

(counts) HFD 12523 ± 970 12386 ± 821

CD control diet; HFD high-fat diet; WT wild-type; Fto-KO Fto-knockout

Weight is indicated as mean ± SEM, metabolic and physical parameters are indicated as mean per day ±

SEM, n = 5–9 per group. P values are obtained with two-way ANOVA and simple main effects analysis

with Bonferroni correction if there was a significant interaction effect (genotype x diet), after which: ap <

0.001 compared with WT mice fed HFD.

5.2 Morphology of white and brown adipose tissue (I, II)

Morphology of eWAT was assessed with hematoxylin-eosin staining and scWAT

and BAT with UCP1-immunostaining (Fig. 9). Of these WAT depots, eWAT

represents a “pure” white adipose tissue as it is not prone to browning under

physiological conditions (164). This is in contrast to scWAT, which is reported to

be the most susceptible to browning (165). In the eWAT, WT mice on HFD showed

enlarged adipocytes, which was not observed in the Fto-KO on HFD. To analyze

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the effect of Fto on browning of WAT, UCP1 protein expression with

immunohistochemistry of scWAT was assessed. In WT mice, adipocytes were

unilocular and mainly UCP1-negative while in Fto-KO scWAT, adipocytes were

multilocular and UCP1-positive. When fed HFD, adipocytes in scWAT of WT mice

were unilocular, hypertrophic and UCP1-negative whereas Fto-KO scWAT, while

containing unilocular and UCP1-negative adipocytes, included also small and

multilocular UCP1-positive cells. In BAT, UCP1 protein was expressed most

highly in Fto-KO mice which was also seen in Ucp1 gene expression (Fig. 14). In

addition, Fto-KO BAT did not accumulate lipid droplets on HFD similar to WT.

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Fig. 9. Hematoxylin-eosin staining of mouse eWAT and UCP1-immunostaining of mouse

scWAT and BAT. WT wild-type; Fto-KO Fto-knockout; eWAT epididymal white adipose

tissue; scWAT subcutaneous white adipose tissue; BAT brown adipose tissue; CD

control diet; HFD high-fat diet. Scale bars are 50 μm (eWAT) and 60 μm (scWAT and BAT).

5.3 Fto gene expression in the WT adipose tissue (I)

To ascertain that the expression of Fto mRNA was absent in the Fto-KO mice, the

relative expression of Fto with RT-qPCR was examined. Fto expression was

undetectable in Fto-KO WAT and BAT depots. Interestingly, a 1.3-fold decrease of

Fto expression in eWAT of WT mice on HFD in comparison to WT on CD was

CD HFD

eWAT

WT

Fto-KO

CD HFD

scWAT

CD HFD

BAT

WT

Fto-KO

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observed (Fig. 10). Furthermore, there was no such dietary effect in scWAT or BAT,

indicating a depot-specific metabolic change. The Fto level was increased by 2.4

fold in scWAT relative to eWAT. It was not possible to compare the expression of

Fto between WAT and BAT depots due to different inter-run controls during RT-

qPCR run setup.

Fig. 10. Relative expression of Fto in WAT and BAT of wild-type mice. eWAT epididymal

white adipose tissue; scWAT subcutaneous white adipose tissue; BAT brown adipose

tissue; CD control diet; HFD high-fat diet. The amount of Fto mRNA was normalized

using Actb and Gapdh as reference genes. Comparison between WAT and BAT depots

is not possible due to experimental conditions. Results are shown as mean ± SEM (n=9

per group). Student’s t-test, **p < 0.01.

5.4 Adipokine production from eWAT (I)

Protein levels of adiponectin and leptin from eWAT of WT and Fto-KO mice are

illustrated in Fig. 11. No difference was observed between WT and Fto-KO mice

on CD; however, adiponectin was reduced by 3.3-fold and leptin increased by 2.7-

fold in WT mice on HFD, the reduction that was not observed in Fto-KO.

eWAT scWAT

0.0

0.5

1.0

1.5

2.0

2.5

3.0

BAT

0.0

0.5

1.0

1.5

2.0

2.5

3.0

Fto

mR

NA

re

lati

ve

to A

ctb

an

d G

ap

dh

HFD CD

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Fig. 11. Protein level of adipokines in eWAT. WT wild-type; Fto-KO Fto-knockout; CD

control diet; HFD high-fat diet. Band intensities were analyzed relative to protein

amount loaded to the gel. All samples were run under the same experimental conditions

and dotted lines indicate the cropping lines. Results are shown as mean ± SEM (n=6 per

group). Two-way ANOVA followed by simple main effects analysis with Bonferroni

correction because of the significant interaction effect, *p < 0.05, **p < 0.01, ***p < 0.001.

5.5 Gene expression related to WAT adipogenesis and function (I)

Relative expression of genes related to adipogenesis and adipose tissue function

were studied in eWAT of WT and Fto-KO mice (Fig. 12). In Fto-KO mice on HFD,

Bmp4 was at the same level as on CD; however, in WT mice on HFD, Bmp4 was

decreased by 2 fold compared with their CD counterparts. Interestingly, there was

no difference between Cebpb expression of WT and Fto-KO eWAT while HFD

consumption was associated with a 1.4- and 1.5-fold increase in Cebpb of WT and

Fto-KO eWAT, respectively.

Relative expression of Cebpa was at the same level between both genotypes

when fed CD; however, HFD introduced a 2.1-fold decrease in Cebpa expression

in WT, which was not observed in Fto-KO mice (Fig. 12). Pparg expression was

1.2-fold higher in Fto-KO mice compared with WT when fed CD. Furthermore, on

HFD Pparg was decreased by 2.2-fold in WT eWAT but only 1.3-fold in Fto-KO.

A similar trend was observed in Rxra expression, a heterodimeric counterpart of

PPARγ. The expression of Glut4 was unaltered between genotypes on CD; however,

HFD decreased the expression by 6.2-fold in WT which was not observed in Fto-

KO.

CD HFD

0.0

0.5

1.0

1.5

2.0

2.5

3.0

Fto-KO WT

Adiponectin

Re

lati

ve b

and

inte

nsi

ty

CD HFD

0.0

0.5

1.0

1.5

2.0

2.5

3.0

Leptin

Adiponectin

Leptin

GAPDH

WT KO WT KO CD HFD

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Fig. 12. Relative expression of genes related to white adipogenesis in eWAT. WT wild-

type; Fto-KO Fto-knockout; CD control diet; HFD high-fat diet. The amount of mRNA

was normalized using Actb and Gapdh as reference genes. Results are shown as mean

± SEM (n=5-9 per group). Two-way ANOVA followed by simple main effects analysis with

Bonferroni correction because of the significant interaction effect or moderation effect,

*p < 0.05, **p < 0.01, ***p < 0.001.

5.6 Gene expression related to browning of WAT and BAT

adipogenesis and metabolism (II)

In the browning process, WAT adipocytes begin to resemble BAT adipocytes and

utilize energy instead of reserving it, resulting in an increase in the expression of

BAT-specific marker genes in the WAT (reviewed in (34)). Relative expression of

BAT-specific genes was analyzed in scWAT of WT and Fto-KO mice, since scWAT

has been shown to be most susceptible to browning in comparison to other WAT

depots (165). As shown in Fig. 13, the expression of Cebpb was increased by 1.4-

fold in Fto-KO mice compared with WT when mice were on HFD. Concurrently,

Pparg was increased by 1.6-fold in Fto-KO on HFD compared with WT. Compared

with mice on CD, the expression of Prdm16 was increased by 1.7-fold in Fto-KO

mice on HFD; this increase was not observed in WT. Adrb3 expression was at the

same level in Fto-KO scWAT fed either of the diets while HFD decreased Adrb3

by 3.1-fold in WT scWAT. The expression of Pgc1a was increased by 3-fold in Fto-

KO on HFD compared with WT on HFD.

Bmp4 CD HFD

0.0

0.2

CD HFD

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Cebpb

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Cebpa CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Pparg CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

mR

NA

re

lati

ve

to A

ctb

an

d G

apd

h

CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Rxra CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Glut4

Fto-KO WT

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Fig. 13. Relative expression of genes related to WAT browning in scWAT. WT wild-type

mice; Fto-KO Fto-knockout mice; CD control diet; HFD high-fat diet. The amount of

mRNA was normalized using Actb and Gapdh as reference genes. Results are shown

as mean ± SEM (n=5-9 per group). Two-way ANOVA followed by simple main effects

analysis with Bonferroni correction because of the significant interaction effect or

moderation effect, *p < 0.05, **p < 0.01, ***p < 0.001.

The relative expression of genes related to adipogenesis and metabolism in BAT of

WT and Fto-KO mice is illustrated in Fig. 14. In the BAT of Fto-KO mice on HFD,

Cebpb expression was increased by 1.3-fold which increase was not observed in

WT. There was no difference in Ucp1 expression between CD-fed mice. However,

it was increased by 1.5-fold in BAT of Fto-KO on HFD; this increase was not

observed in WT. Concurrently, Prdm16 expression was unaltered in Fto-KO mice

on either of the diets, while in WT on HFD its expression was decreased by 1.3-

fold compared with WT on CD. Compared with CD-fed mice, Adrb3 expression

was increased by 1.2- and 1.4-fold in the BAT of HFD-fed WT and Fto-KO mice,

respectively, without significant effect of genotype. The expression of Pgc1a was

increased by 1.4-fold in Fto-KO mice on HFD compared with WT mice.

Cebpb CD HFD

0.0 0.2 0.4 0.6 0.8 1.0 1.2 1.4 1.6

2.4 2.2 2.0 1.8

CD HFD

0.0 0.2 0.4 0.6 0.8 1.0 1.2 1.4 1.6

Pparg

2.2 2.0 1.8

2.4

CD HFD

0.0 0.2 0.4 0.6 0.8 1.0 1.2 1.4 1.6

2.4

Prdm16

2.2 2.0 1.8

CD HFD

0.0 0.2 0.4 0.6 0.8 1.0 1.2 1.4 1.6

Adrb3

2.2 2.0 1.8

2.4

CD HFD

0.0 0.2 0.4 0.6 0.8 1.0 1.2 1.4 1.6

2.4

Pgc1a

2.2 2.0 1.8

Fto-KO WT

mR

NA

re

lati

ve

to A

ctb

an

d G

apd

h

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Fig. 14. Relative expression of genes related to BAT adipogenesis and metabolism in

BAT. WT wild-type mice; Fto-KO Fto-knockout mice; CD control diet; HFD high-fat diet.

The amount of mRNA was normalized using Actb and Gapdh as reference genes.

Results are shown as mean ± SEM (n=5-9 per group). Two-way ANOVA followed by

simple main effects analysis with Bonferroni correction if there was significant

interaction effect or moderation effect, *p < 0.05, **p < 0.01, ***p < 0.001.

5.7 Expression of miRNAs related to adipogenesis and adipose

tissue metabolism (II)

Several miRNAs have been reported to “fine-tune” the expression of genes related

to white and brown adipogenesis as well as browning of WAT (reviewed in (29, 30,

166)). As shown in Fig. 15, the expression of miR-130b, a repressor of Pparg (155)

in scWAT of HFD-fed mice was increased by 2.3-fold in WT but not in Fto-KO

mice. A similar pattern was observed in miR-155, a repressor of Cebpb (156). The

expression of miR-130b was approximately 1.7-fold decreased in BAT of Fto-KO

mice compared with WT irrespective of the diet. The expression of miR-378, which

has been shown to increase Pparg and Glut4 expression (159), was unaltered in

Fto-KO mice fed either of the diets while it showed a 1.4-fold decrease in WT on

HFD when compared with CD.

CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Pgc1a Cebpb CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Ucp1 CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

Prdm16

1.8

CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

1.6

1.8

Adrb3

Fto-KO WT

mR

NA

re

lati

ve

to A

ctb

an

d G

apd

h

effect of diet

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Fig. 15. Relative expression of miRNAs related to beige and BAT adipogenesis. WT wild-

type mice; Fto-KO Fto-knockout mice; CD control diet; HFD high-fat diet. The amount

of miRNA was normalized using SNORD47 and 85 as internal controls. Results are

shown as mean ± SEM (n=4 per group). Two-way ANOVA followed by simple main

effects analysis with Bonferroni correction if there was significant interaction effect or

moderation effect, *p < 0.05, **p < 0.01, ***p < 0.001.

CD HFD

0.0

0.5

1.0

1.5

2.0

2.5

3.0

WT Fto-KO

miR-130b CD HFD

0.0

0.5

1.0

1.5

2.0

2.5

3.0

miR-155 CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

miR-130b CD HFD

0.0

0.2

0.4

0.6

0.8

1.0

1.2

1.4

miR-378

miR

NA

rel

ati

ve t

o S

NO

RD

47

and

85

scWAT BAT

miR

NA

rel

ati

ve t

o S

NO

RD

47

and

85

effect of genotype

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6 Discussion

6.1 Weight development (I)

The results of this study indicate that Fto-KO mice were resistant to diet-induced

obesity. After 16 weeks of dietary experiment, Fto-KO mice on CD weighed as

much as Fto-KO mice on HFD. Weight of WT mice on HFD was significantly

higher compared with mice on CD. Furthermore, food and water intake as well as

activity and energy expenditure were unaltered, which is in line with McMurray et

al. (17) but contradicts with an earlier Fto-deficient mouse model generated by

Fischer et al. (15). Previously published Fto-deficient mouse models differ in the

severity of the phenotype. Generally, mouse models containing a deletion of part

of the Fto gene possess a more severe phenotype with high postnatal mortality and

low body weight from the second postnatal day onwards (15-17). On the other hand,

an Fto-KO mouse model generated by Church et al. with point-mutation inside the

coding region of Fto and without deletion from the genome, possesses more subtle

phenotypic changes such as weight reduction as late as 12 weeks of age onwards

compared with WT and no postnatal mortality (18). The current mouse model was

similar to the latter one as our KO-model terminated Fto mRNA production inside

the second intron without deleting any part of the genome. This allows the

regulation of other genes to occur via non-coding regions of the Fto gene. Indeed,

recent studies indicate that the mechanism in which SNPs within human FTO affect

BMI may be via long-range regulatory alteration of iroquois homeobox 3 and 5

genes IRX3 and 5 (64, 65). IRX family members are important developmental

proteins during regionalization of cell differentiation (reviewed in (167)).

Interestingly, Irx3-deficient mice exhibited reduced body weight from an early age

compared with WT, indicating IRX3 to be also important in energy metabolism

(64).

In this study, only male mice were examined. In previously published Fto-KO

mouse models, males were reported to manifest stronger (15, 17) or similar (16, 18)

phenotype compared with females. Milder phenotype in females unlikely indicate

different mechanism of FTO action between two sexes, but rather reflect the

distinct ability of genders to buffer changes in metabolism and differences in sex

hormone actions in growth and behavior (17). This is supported by the notion that,

opposite to Fto-KO, Fto overexpressing female mice show more pronounced

phenotype than males (20). We observed similar weight development in our Fto-

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KO females than males (data not shown), so we decided to focus on the males only.

However, it is important to examine females in the near future as well. Aside from

metabolic effects of FTO in adults, results from human study indicate that placental

FTO expression is associated with fetal growth, which should be assessed in more

detail with Fto-KO females (11). All reports show that the birth weight of Fto-KO

mice is unaltered; however, usually in the transgenic mouse studies, heterozygous

males and females are used to produce WT, KO and heterozygote pups in the same

litter. With the use of homozygote Fto-KO females, new insights may be revealed

on the role of FTO during intrauterine development. In addition, the effect of

maternal nutrition may be relevant to study, as our results show HFD-dependent

changes in Fto-KO mice which are distinct from WT.

6.2 Adipose tissue morphology (I, II)

Adipocytes were smaller in Fto-KO eWAT, scWAT and BAT after HFD compared

with WT. This is important when the function of FTO in the etiology of obesity and

related diseases is assessed, since the capacity of adipocytes to become

hypertrophic in response to energy intake is key in the pathogenicity of obesity

(168). In addition, the size of adipocytes is highly correlated with the capacity of

adipose tissue to become insulin resistant (169) and pro-inflammatory via various

mechanisms including endoplasmic reticulum stress response (reviewed in (170)).

Indeed, our results indicated an altered adipokine production from Fto-KO eWAT

especially when the mice were fed HFD. In WT mice, adiponectin production was

significantly decreased and leptin increased in HFD-treated mice. This is in

agreement with previous studies that show a dysregulated, inverse relationship of

adiponectin and leptin in obese adipose tissue and serum in humans (171, 172). In

Fto-KO mice on HFD, adipokine production was not altered similar to WT,

indicating a role for Fto in the whole body metabolism and adaptation to changes

in dietary environment. Indeed, serum level of adiponectin was increased and leptin

decreased in the previously published Fto-KO mouse model (15).

Fat mass was not quantified separately from lean mass in the current study. We

are therefore unable to estimate if the weight difference between the Fto-KO and

WT mice is because of altered amount of adipocytes or altered capability of

adipocytes to store the dietary fat. In the light of previous reports, the latter

explanation is more plausible as generally, the fat mass of Fto-KO mice has been

reported to be either reduced (15, 17, 18) or unaltered (16) when compared with

WT. In addition, the International Mouse Phenotyping Consortium database

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(www.mousephenotype. org) indicates that the fat mass of a similar mouse model

presented here (Ftotm1a(EUCOMM)Wtsi) is unaltered (173). Thus, we may postulate that

the fat mass of the current Fto-KO mice is at least not increased. From the unaltered

body and fat mass, unaltered adipocyte area between WT and Fto-KO mice on CD

and the lack of hypertrophy after HFD, we may conclude that the number of

adipocytes is unaltered, and rather that the ability to store dietary fat is challenged

in Fto-KO adipose tissue when the standard conditions are confronted by HFD.

This is in line with Church et al. as they found increased expression of carbohydrate

metabolic genes in muscle of Fto-KO mice and concluded, that it may result from

altered nutrient storage and consequent release from WAT (18). In addition, fatty

acid synthase levels were increased without a change in fat storage in Fto-KO

muscle, indicating a decreased supply of fatty acids from WAT, further supporting

a role for FTO in fat accumulation, which is reduced in Fto-KO contributing to the

lean phenotype of these mice (18). Lack of HFD-mediated downregulation of Glut4

expression in Fto-KO eWAT indicates that FTO may have a role in adipocyte

glucose metabolism since GLUT4 is the main insulin responsive glucose

transporter in adipocytes (reviewed in (174)). Furthermore, adipose tissue-specific

Glut4-deficiency leads to insulin resistance while overexpression contributes to

improved glucose homeostasis (175, 176).

6.3 Effect of HFD on Fto expression in WT mice (I, II)

Interestingly, the relative expression of Fto mRNA was down-regulated in eWAT

of WT mice on HFD, which is in line with previous studies reporting decreased Fto

expression in several mouse models of obesity (13, 72). However, this effect was

not observed in scWAT or BAT, indicating a tissue-specific adaptation to HFD.

Furthermore, Fto level was increased by 2.4 fold in scWAT relative to eWAT. In

mice, eWAT has been reported to be least prone to browning in vivo, thus

representing the “purest” white adipose depot (164). On the contrary, scWAT is

associated with increased browning potential of all WAT depots (165). Thus,

decreased Fto expression in eWAT due to HFD indicates that Fto has a role in the

adaptation of white adipocytes into “obesogenic” environment, while increased Fto

in scWAT relative to eWAT supports a place for Fto also in browning. These results

were further supported by findings from Fto-KO mice, as discussed next in detail.

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6.4 Expression of genes related to white adipogenesis (I)

Observations of morphological changes were further supported by the changes in

gene expression related to white adipogenesis and adipose tissue function in eWAT.

The precise mechanism through which FTO regulates energy balance and the

response to dietary changes is unknown. Our results indicate that the role of FTO

in adipose tissue may be relevant especially in response to HFD as the changes are

more striking in Fto-KO mice on HFD. Genes related to WAT adipogenesis were

expressed higher in the Fto-KO eWAT when stimulated by HFD. Whether these

differences arise from the altered adipogenesis per se or from some other

developmental change before or after adipocyte differentiation cannot be estimated

from the current data. However, these data clearly indicate that Fto has a role in the

adaptation of WAT to environmental changes such as excess dietary fat. Relative

expression of such adipogenesis-related genes as Bmp4, Cebpa, Pparg and Rxra

was significantly decreased in WT mice on HFD; this decrease was not observed

in Fto-KO. A recent study shows that Fto-KO MEFs exhibit decreased mTOR

signaling and mRNA translation with increased autophagy, indicating a role for

FTO in nutrient sensing (77). Furthermore, total inhibition of mTOR prevents 3T3-

L1 preadipocytes from differentiating in mature adipocytes while a partial mTOR

inhibition enhances adipogenesis with increased Pparg and Cebpa expression (177).

Thus, altered mTOR signaling may have contributed to the changes observed in the

current Fto-KO mice.

We found that Fto-deficiency has only a modest effect on gene expression in

each of the adipose tissue depots studied. This could result at least partly from the

nonstoichiometric nature of the m6A modification, which was also observed in

METTL3-depleted mESCs and hESCs (87). METTL3 adds m6A to the consensus

sequence RRACH; however, this consensus sequence occurs more often in mRNA

than m6A residues, indicating that additional sequence or structural features may

be required to define the methylation site (82, 85, 93). Indeed, a recent study reveals

that FTO and ALKBH5 do not actually exhibit strict sequence requirements for

substrate specificity (178). Instead, m6A was suggested to induce a conformational

switch from duplex to hairpin in RNA (and also DNA). This subsequently led to

increased binding ability of FTO, ALKBH5 and possibly other m6A binding

proteins as well (178). Thus, mere sequence analysis may not be sufficient to reveal

FTO targets; it may be necessary to assess the RNA structure as well.

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6.5 Browning of scWAT and BAT adipogenesis (II)

In addition to eWAT, we observed morphological differences also in the Fto-KO

scWAT and BAT depots compared with WT. Adipocytes in scWAT and BAT of Fto-

KO mice on HFD did not exhibit hypertrophy similar to WT mice on HFD. In

addition, immunohistochemical staining of these depots using UCP1-specific

antibody revealed increased UCP1 abundance in Fto-KO scWAT and BAT. The

mitochondrial membrane protein UCP1 is characteristic to BAT adipocytes and is

important in the non-shivering thermogenesis in which heat is generated via

lipolysis rather than ATP (reviewed in (81)). FTO together with CaMKII induces

prolongation of CREB phosphorylation in human neurons, resulting in an

upregulation of genes important in energy metabolism (78). FTO was shown to

directly interact with CaMKII; however, loss-of-function-mutated FTO induced

also a moderate increase in expression of metabolic genes, indicating that FTO’s

demethylase activity does not fully explain the prolonged CREB phosphorylation

(78). Furthermore, CREB phosphorylation has been shown to activate also C/EBPβ

and UCP1 in preadipocytes (80, 81). Our results indicate that lack of Fto leads to

increased Cebpb and Ucp1 expression in scWAT and BAT of HFD-fed mice,

whereas in eWAT the increase of Cebpb was apparent in both genotypes. Thus,

altered CREB signaling may contribute at least partly to the lean phenotype of our

Fto-KO mice via increased scWAT browning and BAT induction. Adipogenesis of

CREB-deficient MEFs is disrupted due to decreased Cebpb expression (80).

However, our results indicate increased Cebpb expression upon Fto-KO, thus the

possible effect of invalidation of Fto on CREB is indirect and compensatory

mechanisms may be present in Fto-KO adipose tissues.

Fto-deficiency was connected to increased Ucp1 and Pgc1a expression in

mouse eWAT and scWAT by Tews et al. with smaller adipocyte size (23). We did

not observe Ucp1 expression in eWAT of any mice, but the results from scWAT and

BAT are in concert with Tews et al. although we did not observe changes on CD.

This discrepancy may be due to the fact that the mice were older in the current

study. We were not able to analyze Ucp1 mRNA expression reliably from scWAT;

however, the immunohistochemistry analysis shows increased UCP1 protein

abundance in Fto-KO mice on HFD, which was also seen in Ucp1 mRNA and

protein of BAT. The reason for incoherent mRNA expressions of Ucp1 in scWAT

is unknown. We analyzed the samples with two to three different primer pairs as

well as with Taqman Gene Expression Assay (ID Mm01244861_m1) and always

received similar results, with expression values differing by 10,000-fold from each

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other regardless of the mouse group. Moreover, we extracted RNA from an

additional scWAT specimens and again, found similar discrepancy with the results.

While UCP1 is an important brown fat marker, PRDM16 has been shown to be

crucial for brown adipogenesis (103). Our results show that Prdm16 expression is

increased in Fto-KO scWAT and BAT after HFD. Furthermore, C/EBPβ co-

operates with PRDM16 to induce BAT differentiation, which subsequently leads to

activation of thermogenic genes such as Adrb3 and Pgc1a, and these genes are also

characteristic to beige adipocytes (179-181). These brown fat markers are increased

in Fto-KO scWAT and BAT after HFD, further supporting enhanced browning and

BAT adipogenesis.

Many miRNAs have been demonstrated to regulate the gene expression related

to white and brown adipogenesis (reviewed in (29, 30, 166)) as well as browning

of WAT (156, 182). In addition, FTO has been shown to participate in the regulation

of certain miRNAs (183). Our results indicate that the adaptation to HFD observed

in the scWAT and BAT of Fto-KO mice may be mediated by miRNAs. MiR-130b

is reported to downregulate Pparg mRNA expression via direct binding (155), and

this effect was present in scWAT of our mice where miR-130b was increased in WT

mice on HFD with concurrent decrease in Pparg expression. In the BAT, the Pparg

expression followed a similar trend without statistical significance (data not shown).

Furthermore, miR-130 is shown to be increased in adipocyte hypertrophy and fat

inflammation (184). MiR-155 is another inhibitor of adipogenesis having direct

interaction with Cebpb mRNA (156). In this study, miR-155 was increased in the

scWAT of WT mice on HFD also with a decrease in the Cebpb expression, which

effect was not observed in Fto-KO scWAT. MiR-378 is upregulated during

adipogenesis and it activates C/EBP transcription factors, including Cebpb (159),

which was seen in the BAT of the current Fto-KO mice after HFD.

6.6 Confounding factors

The current results indicate Fto-dependent changes in murine WAT and BAT, but

do not reveal the developmental onset of these changes. In addition, these changes

are subtle, which may result from the selective nature of m6A modification, i.e. not

all consensus sites are methylated. Another possibility for the subtle changes is the

fact that adipose tissue is a plastic organ and as the mice analyzed here were

relatively old, compensatory effects may have diminished the differences. This was

also speculated to be a confounding factor in the study by Church et al. in which

adult Fto overexpressing mice were investigated; the analysis was thus carried out

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after the body weight had already diverged (20). Indeed, human studies indicate a

stronger effect of FTO SNPs on BMI in younger individuals and also an association

between placental FTO mRNA expression and fetal weight (11, 44, 72). Thus, it is

important to analyze the effects of Fto-KO on different developmental phases from

early embryonic days onwards.

This study, as well as most of mouse studies, was conducted with mice that

were housed at room temperature (~21°C). However, there is growing evidence

that this temperature, while being optimal for humans, is too cold for mice

(reviewed in (185)). Main problem with the housing at room temperature is that it

is well below mouse thermoneutral zone (~30°C) i.e. mice need to increase their

metabolic rate above basal metabolic rate to maintain their core body temperature.

This may be problematic when BAT and browning are under investigation since

main function of these tissues is thermogenesis. In addition, if the results obtained

from mouse studies are eventually going to be translated to human biology, the

problem arise from the fact that generally, humans live within their thermoneutral

zone with the help of clothes and heating systems (185). Indeed, Ucp1-KO mice

exhibit obese phenotype when housed at thermoneutrality, but not at room

temperature (186).

6.7 Future prospects

The mechanism by which FTO acts in placenta is not clear and the effects of FTO

during pre- and post-natal development should be assessed in more detail.

Environmental factors such as mothers eating behavior during pregnancy are

known to affect the epigenetics and lifelong development of a child and FTO may

have a role in this as well. Furthermore, detailed assessment of gene-environment

interactions will broaden our understanding of the genetics behind obesity and the

role of FTO in it. The physiological significance of m6A modification is only

currently being resolved and the specificity of m6A demethylase activity of FTO is

still obscure. The current study indicates a role for FTO in adipose tissue plasticity

via miRNA regulation. Several studies predict miRNA target sites with subsequent

binding experiments; however, the presence and consequence of such

modifications as m6A in the miRNA binding site are yet to be identified. It is thus

crucial to investigate the precise mechanism of m6A actions in the near future. In

addition to FTO, one other m6A demethylase, ALKBH5, has been identified. The

existence of additional m6A demethylases is plausible and an important question

to be answered.

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6.8 Summary

From the current results, it is difficult to estimate, which came first in Fto-KO mice,

the improved adipokine production or decreased body weight on HFD. What is

clear however, is that these mice do not develop diet-induced obesity despite

unaltered energy intake, heat production, respiratory exchange ratio and activity

relative to WT. While adipocytes do not become larger on HFD, where does the

excess energy go? Whether the issue is about nutrient absorption or accumulation

of fat into other peripheral tissues remains to be answered. Results of the current

study are summarized in the Fig. 16.

Fig. 16. Altered response of Fto-deficient adipose tissue to high-fat diet. In wild-type

mice, FTO decreases the levels of genes related to adipogenesis while promoting

adipocyte hypertrophy and obesity with unhealthy consequences. In Fto-deficient mice,

genes related to adipogenesis remain elevated after high-fat diet which prevents

adipocytes from becoming hypertrophic and improves overall metabolic performance.

miR-378

miR-130 miR-155

Pparg Cepba Rxra

Bmp4

FTO

High-fat diet

Pparg Cepba Rxra

Bmp4 miR-130 miR-155 miR-378

Wild-type adipose tissue

Fto-deficient adipose tissue

RNA methylation?

FTO

High-fat diet

Small adipocytes

Adipocyte hypertrophy

LeptinInsulin resistance? Inflammation?

mTOR, nutrient sencing? CREB signaling?

AdiponectinBrowningInsulin sensitive?

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7 Concluding remarks

The findings of this thesis are as follows:

1. Fto-deficient mice were resistant to diet-induced obesity and adipocyte

hypertrophy while energy intake, heat production, respiratory exchange ratio

and physical activity were unaltered relative to wild-type.

2. Adaptation to high-fat diet was altered in the Fto-deficient adipose tissues.

Expression of genes related to white and brown adipogenesis and function as

well as browning were not attenuated as a response to high-fat diet similar to

wild-type. Thus, in the wild-type mice FTO regulated these genes in response

to dietary fat while this regulation was absent in Fto-deficient mice.

3. Expression of microRNAs that are previously reported to regulate genes

related to above-mentioned processes was altered in the Fto-deficient mice.

This indicated that FTO regulated the adipose tissue adaptation to high-fat diet

via microRNA regulation.

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144. Oishi Y, Manabe I, Tobe K, Tsushima K, Shindo T, Fujiu K, Nishimura G, Maemura K, Yamauchi T, Kubota N, Suzuki R, Kitamura T, Akira S, Kadowaki T & Nagai R (2005) Kruppel-like transcription factor KLF5 is a key regulator of adipocyte differentiation. Cell Metab 1(1): 27-39.

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151. Karbiener M, Pisani DF, Frontini A, Oberreiter LM, Lang E, Vegiopoulos A, Mossenbock K, Bernhardt GA, Mayr T, Hildner F, Grillari J, Ailhaud G, Herzig S, Cinti S, Amri EZ & Scheideler M (2014) MicroRNA-26 family is required for human adipogenesis and drives characteristics of brown adipocytes. Stem Cells 32(6): 1578-1590.

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153. Karbiener M, Fischer C, Nowitsch S, Opriessnig P, Papak C, Ailhaud G, Dani C, Amri EZ & Scheideler M (2009) microRNA miR-27b impairs human adipocyte differentiation and targets PPARgamma. Biochem Biophys Res Commun 390(2): 247-251.

154. Wu Y, Zuo J, Zhang Y, Xie Y, Hu F, Chen L, Liu B & Liu F (2013) Identification of miR-106b-93 as a negative regulator of brown adipocyte differentiation. Biochem Biophys Res Commun 438(4): 575-580.

155. Lee EK, Lee MJ, Abdelmohsen K, Kim W, Kim MM, Srikantan S, Martindale JL, Hutchison ER, Kim HH, Marasa BS, Selimyan R, Egan JM, Smith SR, Fried SK & Gorospe M (2011) miR-130 suppresses adipogenesis by inhibiting peroxisome proliferator-activated receptor gamma expression. Mol Cell Biol 31(4): 626-638.

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157. Sun L, Xie H, Mori MA, Alexander R, Yuan B, Hattangadi SM, Liu Q, Kahn CR & Lodish HF (2011) Mir193b-365 is essential for brown fat differentiation. Nat Cell Biol 13(8): 958-965.

158. Mori M, Nakagami H, Rodriguez-Araujo G, Nimura K & Kaneda Y (2012) Essential role for miR-196a in brown adipogenesis of white fat progenitor cells. PLoS Biol 10(4): e1001314.

159. Gerin I, Bommer GT, McCoin CS, Sousa KM, Krishnan V & MacDougald OA (2010) Roles for miRNA-378/378* in adipocyte gene expression and lipogenesis. Am J Physiol Endocrinol Metab 299(2): E198-206.

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186. Feldmann HM, Golozoubova V, Cannon B & Nedergaard J (2009) UCP1 ablation induces obesity and abolishes diet-induced thermogenesis in mice exempt from thermal stress by living at thermoneutrality. Cell Metab 9(2): 203-209.

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Original publications

I Ronkainen J, Huusko TJ, Soininen R, Mondini E, Cinti F, Mäkelä KA, Kovalainen M, Herzig KH, Järvelin MR, Sebért S, Savolainen MJ & Salonurmi T (2015) Fat mass- and obesity-associated gene Fto affects the dietary response in mouse white adipose tissue. Sci Rep 5:9233.

II Ronkainen J, Mondini E, Cinti F, Cinti S, Sebért S, Savolainen MJ & Salonurmi T (2016) Fto-deficiency affects the gene and microRNA expression involved in brown adipogenesis and browning of white adipose tissue in mice. Manuscript.

Original publications are not included in the electronic version of the dissertation.

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ROLE OF FTO IN THE GENE AND MICRORNA EXPRESSION OF MOUSE ADIPOSE TISSUES IN RESPONSE TO HIGH-FAT DIET

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