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David P. Siderovski, Ph.D.

Ph.D. in Medical Biophysics, University of Toronto, under Dr. Tak W. Mak HIV-1 Transcriptional Regulation, 1997

B.Sc. (Honours) in Biochemistry, Queen’s University – Kingston, ON, under Dr. Don ForsdykeCloning of G0S8 / RGS2, 1989

Professional Experience: 2017 – present Chair of the Department of Physiology, Pharmacology & Neuroscience 2015 – present Co-Director of Basic Research, WVU Addictions Research Group,

WVU Health Sciences Center, West Virginia University, Morgantown, WV 2014 – present Director, MD/PhD Dual Degree Scholars Program,

WVU School of Medicine, West Virginia University, Morgantown, WV 2012 – present E.J. Van Liere Endowed Medicine Professor, and

Chair of the Department of Physiology and Pharmacology, WVU School of Medicine, West Virginia University, Morgantown, WV

2009 – 2012 Professor, and Director of Chemical Biology, Department of Pharmacology, University of North Carolina at Chapel Hill

2006 – 2012 Thomas J. Dark Director of Basic Research for the UNC MD/PhD Program 2004 – 2008 Associate Professor (tenured), UNC Department of Pharmacology 1999 – 2004 Assistant Professor (tenure-track), UNC Department of Pharmacology 1994 – 1999 Head of the Quantitative Biology Laboratory,

Amgen Institute & AMGEN Inc., Thousand Oaks, CA Highlights: Ø Discovered the RGS protein family, leading to four issued patents, ten books

and book chapters, twenty-nine review articles, editorials, and letters-to-the-editor,over one hundred peer-reviewed research articles, and >19,500 citations( http://www.ncbi.nlm.nih.gov/pubmed/?term=siderovski+d+%5Bauthor%5D )

Ø Secured over $14 million in direct research support from the National Institutes ofHealth, as well as additional research funding from corporate and private sponsors includingBellBrook Labs, Broad Institute (Harvard/MIT), Burroughs Wellcome Trust, and Coca-Cola.

Ø As Chair for six years at the West Virginia University School of Medicine,Merged faculty, resources, and responsibilities across three distinct departments ofPhysiology, Pharmacology, and Neurobiology into a single department;Hired four new, successful faculty members (an Assistant Professor from the NationalInstitute of Mental Health, an Assistant Professor and an Associate Professor from U.Pittsburgh, and an Assistant Professor from the NIEHS, RTP, NC); andGuided three WVU Assoc. Professors to full Professor via the Promotion & Tenure process.

Ø Successfully led the Diversity and Institutional Setting components of reaccreditationfor West Virginia University School of Medicine, culminating in a full eight-year unconditionalaccreditation from Liaison Committee on Medical Education (2015 – 2023).

Ø Successfully led UNC’s MD/PhD Program to second in the nation in NIH F30 NRSAfellowships held by trainees (2006 – 2012); currently directing the WVU MD/PhD Program(2014 – present) with multiple scholars finishing their PhD phases with 2-year or 3-yeardissertations.

CV of David P. Siderovski, Ph.D. – June 2018 (page 2)

Honors and Awards:

2006 Phillip and Ruth Hettleman Prize for Outstanding Scholarly Achievement, UNC-Chapel Hill, North Carolina

2004 John Abel Award to the Outstanding American Pharmacologist under 40, American Society for Pharmacology & Experimental Therapeutics (ASPET)

2004 Seventeenth Charles W. Gowdey Distinguished Lecturer, Dept. of Physiology & Pharmacology, University of Western Ontario

2001 - 2004 New Investigator Award -- Basic Pharmacological Sciences, Burroughs-Wellcome Fund, Research Triangle Park, NC

2001 - 2003 Year 2000 EJLB International Neuroscience Research Scholarship, The EJLB Foundation, Montréal, Québec, Canada

Four Patents:

“Using lung or bronchial epithelial cells to identify bitter taste modulators”; United States Patent 9,128,079. Radhakrishna, Brown, Siderovski, Kimple, Cohen.

“Apoptosis-Inducing Factor”; United States Patents 6,773,911 and 7,371,834. Penninger, Kroemer, Siderovski, Zamzami, Susin, & Snow.

“Methods of Inhibiting Syp Binding to a CTLA-4 Receptor”; United States Patent 5,786,152. Marengere, Siderovski, & Mak.

Professional Service:

National Institutes of Health (NIH) study-sections

2018 Member, OTC SBIR/STTR panel, Cancer Drug Devel. & Therapeutics, NIH/CSR 2016, 2018 Member, ZGM1 TRN-7, Special panel review of MIRA applications, NIH/NIGMS 2015 Member, ZRG1 MDCN-R, “Biochemistry Special Emphasis Panel”, NIH/CSR 2015 Member, ZRG1 F05-D, “Cell Biology, Dev. Biology & Bioengineering”, NIH/CSR 2014 Member, ZRG1 MDCN-N, “Mol. Neurosci. Special Emphasis Panel”, NIH/CSR 2013 Member, ZDA1 SXC-E, “Cutting-Edge Basic Research Awards (R21)”, NIH/NIDA 2013 Acting Chair, Special Emphasis Panel “Understanding Functions of

Uncharacterized Genes in Infectious Disease Pathogenesis”, NIH/NIAID 2010 – 2012 Biomedical Research & Research Training cmte A (BRT-A), NIH/NIGMS 2009 – 2010 Chairperson, Roadmap HTS Assay Development (BST-J 51), NIH/CSR 2006 – 2010 K99/R00 Pathway to Independence Study Section, NIH/NIGMS 2009 ARRA P30 Faculty Start-up Funds award review panel, NIH/NIGMS 2008 – 2009 High Throughput Screening (BST-Q 50) Study Section, NIH/CSR 2005 – 2009 Cell Biology Fellowship (F05) Study Section, NIH/CSR 2005 – 2006 Allergy, Immunology & Transplantation Research committee, NIH/NIAID 2004 Synapses, Cytoskeleton & Trafficking (SYN), NIH/CSR 2002 Cell Development and Function 3 (CDF3) Study Section, NIH/CSR National Science Foundation (NSF) panels 2007 Signal Transduction & Cellular Regulation Panel member (ad hoc) Scientific meeting organization 2004 Co-organizer (with Dr. Doron Lancet, Weizmann Inst., Israel) G-Protein Signaling Symposium, ELSO, Nice, France 2004 Co-organizer (with Dr. Vadim Arshavsky, Harvard Univ./MEEI) 2nd RGS Protein Colloquium, Washington, DC


Professional societies 2007 – 2008 Chair, ASPET John J. Abel Award Selection Committee 2006 Member, ASPET John J. Abel Award Selection Committee 1998 – present Member, American Society for Biochemistry and Molecular Biology 1998 – present Member, American Society for Pharmacology & Experimental Therapeutics Consultancies 2017 – present Scientific Advisory Board, BellBrook Labs, Madison, WI 2007 – 2013 Biosciences, The Coca-Cola Co., Atlanta, GA 2001 – 2003 Scientific Advisory Board, Wyeth-Ayerst CNS Group, Princeton, NJ 2000 – 2002 Inspire Pharmaceuticals Inc., Durham, NC

Editor 2013 – present Editorial Board member, Journal of Biological Chemistry 2003 – 2004 Editor, “Regulators of G-Protein Signaling” series of Methods in Enzymology, Academic Press (Elsevier Press) 2002 – present RGS Nomenclature Specialist, Human Genome Organisation, UK 2007 – 2008 Guest Editor, Two issues of Comb. Chem. High-Throughput Screening 2001 – 2006 Associate Editor, Molecule Pages, AfCS/Nature Publishing Group

Editorial review (ad hoc)

AJP-Cell Physiology, Analytical Chemistry, Biochemistry, Biochimie, Brain Research, Cell Cycle, EMBO J., European J. of Neurosci., FEBS Letters, Fungal Genetics & Biology, Genomics, J. Biol. Chem., J. Cell. Physiology, J. Neurochem., J. Neurosci., Mol. Pharmacology, Nature Cell Biol., Nature Medicine, Nature Neuroscience, Neuropsychopharmacology, Neuroscience, Nucleic Acids Res., Oncogene, Proc. Natl Acad. Sci., Science, Structure, Transgenic Research, Trends in Biochemical Sciences, Trends in Cell Biology, Trends in Pharmacological Sciences

Seminars Presented:

Oral presentations at national and international scientific meetings

September 2016 Sturge-Weber Foundation and SWF International Research Network Mtg, Atlanta, Georgia September 2014 XXIVth Int’l Conf. of European Chemoreception Research Organization Dijon, France November 2011 6th Annual GPCR-Based Drug Discovery meeting, Cambridge Healthtech Institute, Boston, MA April 2011 RGS & AGS Proteins in Physiology and Disease, ASPET/EB 2011, DC December 2010 Molecular Pharmacology of G Protein-Coupled Receptors 2010, Monash University, Victoria, Australia October 2009 10th Annual Great Lakes GPCR Retreat, Rochester, NY April 2009 15th Annual Society for Biomolecular Screening, Lille, France June 2007 Gordon Research Conference: Phosphorylation and G-Protein Mediated Signaling Networks, Biddeford, ME April 2006 ASBMB/Experimental Biology 2006, San Francisco, CA October 2005 Great Lakes GPCR Retreat, Montebello, Québec, Canada June 2005 67th Annual Mtg, College on Problems of Drug Dependence, Orlando, FL June 2005 Gordon Research Conference: Second Messengers and Phosphoproteins, Biddeford, ME May 2005 Gordon Research Conference: Molecular Pharmacology, Pisa, Italy April 2005 International Congress on Schizophrenia Research, Savannah, GA


September 2004 Speaker and Co-organizer (with Dr. Doron Lancet, Weizmann Inst.) G-Protein Signal Symposium, Euro. Life Sci. Organisation, Nice, France August 2004 12th International Conference on Second Messengers and Phosphoproteins, Montréal, Québec, Canada May 2004 47th Annual CSBMCB Meeting: Cellular Signalling – From the Plasma Membrane to the Nucleus, Mt. Tremblant, QC, Canada April 2004 Speaker and Co-organizer (with Dr. Vadim Arshavsky, Harvard) 2nd RGS Protein Colloquium, Exp’tal Biology 2004, Washington, DC June 2003 Gordon Research Conference: Second Messengers and Protein Phosphorylation, Meriden, NH April 2002 G-Protein Signaling Workshop, Mount Sinai Hospital, NYC, NY October 2001 2nd EJLB Scholar Symposium, North Hatley, Québec, Canada December 2000 Macromolecules in Signal Transduction, Amer. Chem. Soc., New Orleans October 2000 11th International Congress of Endocrinology, Sydney, Australia June 2000 RGS Protein Colloquium, ASBMB/ASPET Joint Mtg, Boston, MA November 1999 Great Lakes GPCR Retreat, London, Ontario, Canada April 1999 Pharmacology ’99 at Exp. Biol. ’99, ASPET/FASEB, Wash., DC March 1999 Merck-Frosst G-Protein Coupled Receptor Retreat, Montréal, QC February 1999 Gordon Research Conference: Mol. Pharmacology, Ventura, CA

Invited external seminars

June 2015 Stanley Center for Psychiatric Research, Broad Institute of MIT and Harvard University, Cambridge, MA

September 2014 Temasek Life Sciences (TLL), National University of Singapore, Singapore February 2013 Stanley Center for Psychiatric Research, Broad Institute of MIT and

Harvard University, Cambridge, MA June 2012 Lilly Research Laboratories, Eli Lilly & Co., Indianapolis, Indiana December 2010 Temasek Life Sciences (TLL), National University of Singapore, Singapore December 2010 Duke-NUS Graduate Medical School, Singapore April 2010 Novartis main campus, Basel, Switzerland December 2009 Department of Pharmacology, Loyola University Stritch School of Medicine,

Chicago, IL March 2009 Skaggs School of Pharmacy & Pharmaceutical Sciences, San Diego, CA December 2008 South Carolina College of Pharmacy, Charleston, SC December 2008 Duke Eye Center, Duke University Medical School, Durham, NC November 2008 Department of Pharmacology, UCSD, San Diego, CA October 2008 Department of Physiology and Biophysics,

Weill Medical College of Cornell University, New York, NY October 2008 Department of Structural & Chemical Biology,

Mount Sinai School of Medicine, New York, NY May 2008 Institute of Molecular Medicine & Genetics,

Medical College of Georgia, Augusta, GA September 2007 Dept. of Pharmacology, University of Minnesota, Twin Cities, MN May 2007 Dept. of Cell Biology & Anatomy, University of Calgary, Calgary, AB March 2006 Institute for Research in Immunology and Cancer, September 2004 Inst. of Mol. Biotechnology, Austrian Academy of Sciences, Vienna, Austria May 2004 Dept. of Pharmacology, Univ. of Illinois at Chicago, Chicago, IL April 2004 Dept. of Physiology & Pharmacology, Univ. of Western Ontario, London, Ontario, Canada


December 2003 Dept. of Pharmacology & Toxicology, Medical College of Georgia, Augusta, GA August 2002 Dept. of Functional Genomics, GlaxoSmithKline, RTP, NC November 2001 Depts. of Biochemistry & Mol. Biol. and Molecular Genetics, M.D. Anderson Cancer Center, Houston, TX October 2001 Kimmel Cancer Institute, Thomas Jefferson Univ., Philadelphia, PA May 2001 Dept. of Mol. Pharm. & Biol. Chem., Northwestern Univ., Chicago, IL May 2001 Dept. of Med. Chem. & Mol. Pharm., Purdue University, West Lafayette, IN April 2001 Dept. of Pharmacology and Cancer Biology, Duke University, Durham, NC April 2001 Dept. of Pharmacology, Weill Medical College of Cornell University, NY, NY March 2001 Wyeth Neuroscience, Wyeth-Ayerst Research, Princeton, NJ February 2001 Neuroscience Group, Pfizer Inc., Groton, CT November 2000 Dept. of Pharmacology, University of Michigan, Ann Arbor, MI June 2000 Dept. of Pharmacology, Yale University, New Haven, CT November 1999 Department of Lab Medicine & Pathobiology, Univ. of Toronto, Canada November 1999 Hospital for Sick Children Research Institute, Toronto, ON, Canada November 1999 National Institute of Environmental Health Sciences, RTP, NC July 1999 Merck Research Laboratories, Merck Inc., Rahway, NJ Invited, local campus seminars

July 2014 Alexander B. Osborn Hematopoietic Malignancy & Transplantation Program, “RGS12: Dynamic scaffold for oncogenic Ras & Raf critical to myoblasts”

September 2012 WVU Health Sciences Center Graduate Student Organization “Regulator of G protein Signaling (RGS) proteins: Swimming back

from Big Pharma”

September 2012 WVU Center for Neuroscience “Disrupting RGS Protein Expression Impairs Cortico-striatal Circuitry”

May 2011 UNC School of Medicine, Department of Cell & Molecular Physiology “Physiological control of GPCR actions in cardiovascular, respiratory, and

CNS circuits by RGS proteins” [Internal Candidate for open Chair position]

February 2011 UNC School of Medicine, Department of Pharmacology “Regulators of G-protein Signaling: An Update”

October 2009 UNC School of Pharmacy “GTPase acceleration as the sole determinant of GPCR kinetic

sharpening by ‘regulator of G-protein signaling’ (RGS) proteins”

September 2007 UNC School of Dentistry, Center for Neurosensory Disorders “RGS Proteins: Novel Targets for Drug Discovery”

April 2007 UNC Hettleman Prize Lecture (George Watts Hill Alumni Center) “Regulators of G-protein Signaling: New Targets for Drug Discovery”

April 2006 UNC School of Medicine Biophysics Training Program “Peptide modulators of Ga subunits: Structural & functional studies”

November 2005 UNC School of Medicine Roadmap Initiative Information Seminar “Responding to NIH Roadmap HTS screening RFA-RM-06-004” November 2004 UNC School of Medicine, Department of Pharmacology “Mechanistic studies of a novel Ga nucleotide cycle underlying mitotic spindle force generation”


March 2003 UNC Mini Medical School (Friday Center) “Protein Crosstalk & Crystal Structures for Drug Targets” December 2001 UNC Hospitals Neurology Grand Rounds “RGS Proteins: Unveiling New Frontiers in GPCR Signaling”

November 2001 UNC School of Medicine, UNC Neuroscience Center “RGS Proteins: Unveiling New Frontiers in GPCR Signaling” Academic Service:

WVU committees 2015 – present Chair, WVU Substance Abuse Task Force - Research Sub-committee 2014 Chair, Faculty Search Committee for Neuro-immunology Position,

WVU Dept. of Microbiology, Immunology and Cell Biology 2013 – 2015 Chair, LCME Standards “Diversity” & “Institutional Setting” Committees 2012 – 2018 Member, WVU Center for Neuroscience (CfN) Steering Committee UNC-Chapel Hill committees 2011 – 2012 Member, Task Force 2 (“Research Platforms”), UNC SoM Strategic Plan 2007 – 2012 Chair, School of Medicine Biochem. Cores Advocacy Committee 2008 School of Medicine Structural Biology Core Facility Search Cmte (Dr. Edward Collins, chair) 2007 – 2008 Department of Pharmacology/Lineberger Comprehensive Cancer

Center Faculty Search Committee (Dr. Gary Johnson, chair) 2005 – 2012 School of Medicine MD/PhD Program Exec. Advisory Committee, (Dr. Gene Orringer, chair) 2004 – 2007 School of Medicine Dean’s Research Advisory Committee, (Dr. Bill Marzluff, chair) 2005 – 2006 School of Medicine Translational Research Advisory Committee, (Dr. Gene Orringer, chair) 2001 – 2005 Chair of the Avery Steelman Lectureship Selection Committee, UNC-Chapel Hill School of Medicine 2001 – 2002 School of Medicine Bioinformatics Faculty Search Committee (Dr. Charles Carter, chair) 2000 – 2001 College of Arts & Sci. Bioinformatics Faculty Search Committee (Dr. Douglas G. Kelly, chair) 2000 – 2001 Dept. of Pharmacology Bioinformatics Faculty Search Committee (Dr. T. Kendall Harden, chair) 1999 – 2000 College of Arts & Sci. Bioinformatics Faculty Search Committee (Dr. Greg Forest, chair) Committees at other institutions 2007 Laboratory of Signal Transduction Staff Scientist Search Committee National Inst. of Environmental Health Sciences, RTP, NC

(Dr. William Copeland, chair) 2006 External 5-Year Review Board panelist, Robarts Research Institute University of Western Ontario, London, ON, Canada (Dr. Serge Carrière, chair)


WVU Teaching Record:

Graduate Medical Education course lectures

2016 - present Lecturer, GME Resident Training: ‘Pharmacology, Brain Fcn. & Behavior’, WVU Department of Behavioral Medicine and Psychiatry “Anxiolytics” (1 hr lecture) 2014 - 2015 Lecturer, GME Resident Training: ‘Pharmacology, Brain Fcn. & Behavior’, WVU Department of Behavioral Medicine and Psychiatry “Anti-Depressants; Anxiolytics; Anti-Psychotics; Advanced Topics” (Four 1 hr lectures)

Professional student course lectures

2014 - 2016 Lecturer, PCOL-743 Pharmacy Pharmacology “Cholesterol & Pharmacological Regulation of Plasma Lipids” (1 hr lecture) 2013 - present Lecturer, PCOL-801 Medical Pharmacology “Inflammation, Glucocorticoids, NSAIDs” (3 hrs of lectures) “Mucociliary Clearance Drugs” (1 hr lecture) “Androgens” (1 hr lecture) “Asthma & Anti-asthma Drugs” (2 hrs of lectures) “Control of Plasma Lipids” (1 hr lecture) “Antidepressants; Anxiolytics; Drugs for Bipolar & ADHD” (4 hrs of lectures) “General Anesthesia” (2 hrs of lectures) “Anticonvulsants” (1 hr lecture) 2012 - 2016 Lecturer, PCOL-760 Dental Pharmacology “Pharmacological Control of Plasma Lipids” (1 hr lecture)

Graduate student course lectures

2014 - present Lecturer, BMS793A Foundations for Contemporary Biomedical Research “Prokaryotes vs. Eukaryotes” (1 hr lecture); “Parkinson’s Disease / Schizophrenia” (two 1 hr lectures); “Pathogenesis: Atherosclerosis” (1 hr lecture) 2014 - present Lecturer, BMS793B Foundations for Contemporary Biomedical Research “Lipids & Steroids / Estrogen receptor & cancer” (two 1 hr lectures) 2014 - present Lecturer, PCOL-449/549 Drugs & Medicine / Applied Pharmacology “General Anesthetic Agents” (1 hr lecture) 2013 - present Lecturer, CCB701/BIOC791E Biochemical & Oncogenic Signaling “G protein coupled receptors; Week 5” (two 90 min lectures)

UNC Teaching Record:

Graduate course direction

2009 – 2011 Course Director, PHCO-732 “Grant-Writing Class” 2008 – 2009 Course Director, PHCO-701; Fall semester course “Receptors: Introduction to Molecular Pharmacology” 2004 – 2007 Course Co-Directorship (with Dr. JoAnn Trejo) of PHCO-701 (formerly PHCO-201); Fall semester course

Graduate course lectures

2004 – 2012 Lecturer, PHCO-701 (formerly PHCO-201); Fall semester course “Receptors: Introduction to Molecular Pharmacology” Block Leader of “Genes to Proteins/Mol. Biol.” and two lectures: “Introduction to Bioinformatics I & II”


2005 – 2012 Lecturer in MS2 Medical Pharmacology, Block 7 (CNS) General Anesthetic Agents, Anxiolytics, Sleep/Hypnotic Agents 2000 – 2012 Lecturer in PHCO-644 (formerly PHCO-118), “G-Protein Coupled Receptors” (90 minute lecture) “Heterotrimeric G-proteins” (90 minute lecture) “Cbl Structure - Meng et al. Nature ‘99” (Discussion Leader) 2007 – 2009 Lecturer, “Ethics in Peer Review” (for all 1st year graduate students) 2000 – 2008 Lecturer in PHCY-412 (formerly PHCY-68), Pharmacodynamics “Signaling by G-Protein Coupled Receptors – Parts I & II” 2005 – 2006 Lecturer in MS2 Medical Pharmacology, Block 7 (CNS) “Anti-Psychotic Drugs; Parkinson’s Disease & other Movement Disorders” 2001 – 2004 Lecturer in PHCO-202, Principles of Pharmacology and Toxicology “Special Research Topic: Regulators of G-Protein Signaling” 2001 – 2004 Lecturer in PHCO-56, CNS/Chemotherapy “Parkinson’s Disease and other Movement Disorders” “General Anesthetic Agents” and “Anti-epileptic Drugs” 2001 Lecturer in PHCO-221B, Signal Transduction “Structural Biology of G-Protein Signaling” 1999 Lecturer in PHCO-117, Cell Structure, Signaling, Growth Control “RGS Proteins - Berman et al. JBC ‘96” (Discussion Leader)

MD/PhD student lectures 2007 – 2012 Course Director, “F30/F31 Fellowship Application ‘Boot Camp’ ”

Undergraduate student lectures 2003 – 2012 Lecturer, Carolina Summer Fellows, “From Industry Back to Academia”

Graduate courses at other institutions Sept. 2014, Lecturer in BL5223, Advanced Molecular Genetics in the Oct. 2005, Temasek Life Sciences Graduate Student Program, Oct. 2003 National University of Singapore “Protein Folds and Function” & “Signaling Cascades in Eukaryotes”

Training grant direction 2006 – 2012 Co-Director, UNC Medical Scientist Training Program, T32 GM008719, National Inst. of General Medical Sciences

Ph.D. student preceptorships 2016 – present Shane Kaski, B.S., WVU Dept. of Physiology & Pharmacology 2014 – present Joshua Gross, B.S., WVU Dept. of Physiology & Pharmacology 2014 – present Adam Schroer, M.S., WVU Dept. of Physiology & Pharmacology 2013 – 2016 Bryan J. Gall, B.S., WVU Dept. of Physiology & Pharmacology 2009 – 2013 Dustin Bosch, B.S., UNC Department of Pharmacology 2007 – 2010 Stephanie Q. Hutsell, M.S., UNC Biophysics Program 2006 – 2010 Adam Kimple, B.S., M.S., UNC Department of Pharmacology 2004 – 2007 Christopher Johnston, Pharm.D., UNC Department of Pharmacology 2002 – 2006 Melinda Willard (nee Hains), B.S., UNC Department of Pharmacology 2000 – 2005 Randall J. Kimple, B.S., UNC Department of Pharmacology

Postdoctoral supervision

2009 – 2013 Dr. Staci Padove Cohen, Ph.D. 2008 – 2012 Dr. Emily Oestreich, Ph.D.


2007 – 2012 Dr. Patrick Giguere, Ph.D. 2007 – 2011 Dr. Genevieve Laroche, Ph.D. 2006 – 2007 Dr. Liu Hao, Ph.D. 2002 – 2007 Dr. Francis S. Willard, Ph.D. 2003 – 2005 Dr. Christopher McCudden, Ph.D. 2001 – 2005 Dr. Miller B. Jones, Ph.D. 2001 – 2002 Dr. Adam Shutes, Ph.D. (co-mentored with Channing Der, UNC) 1999 – 2000 Dr. Bonita Blake, D.V.M., Ph.D. (co-mentored w/ Richard Mailman, UNC)

K-series NIH award mentorship duties

2007 – 2011 Dr. Teresa Tarrant, M.D. (K08 AI070684) 2000 – 2003 Dr. Bonita L. Blake, D.V.M., Ph.D. (K01 MH001896) Selected List of External Research Support

6045290-5500000556 Siderovski (PI) 7/01/13 – 6/30/14 Stanley Center for Psychiatric Research/Broad Institute Subaward Investigations of RGS proteins in the etiology of schizophrenia The Siderovski laboratory shares an interest with the Stanley Center for Psychiatric Research in exploring the role of RGS proteins in schizophrenia toward developing novel pharmacotherapy for this chronic, severe, and disabling brain disorder. There is potential for identifying first-in-class, RGS protein directed small molecule modulators, even while the primacy of G protein-coupled receptors (GPCRs) as drug discovery targets is undeniable. [No code] Siderovski (PI) 12/01/07 – 12/31/13 Coca-Cola Inc. Investigations of tastant receptor signaling in immortalized human lung airway cell lines The molecular basis for taste has been established as tastant stimulation of particular T1R or T2R G protein-coupled receptors on lingual taste bud cells. These discoveries provide new, unprecedented opportunities for manipulating the physiological timing and duration of sweet, bitter, and umami gustation to the benefit of identifying novel tastants or taste enhancers. We are working to ascertain whether this new knowledge of the molecular determinants of taste perception can be used to establish screening assays for novel sweetness enhancers, inhibitors of tastant linger, and/or bitter off-taste reducers. R01 GM082892 Siderovski (PI) 8/01/08 – 7/30/13 NIH/NIGMS Structural determinants of heterotrimeric G-protein nucleotide cycling Major goals are to define the structural determinants underlying nucleotide exchange exhibited by select G-alpha subunits, to discern the non-GAP functions of RGS proteins in GPCR signal regulation, and to define the connectivity between GPCR intracellular loops and heterotrimeric G-protein subunits by x-ray crystallography. R01 CA127152 Der (PI) 4/01/07-3/31/12 NIH/NCI Role of RGS Proteins in Ras- and B-Raf-Mediated Transformation We hypothesize that subfamily-D RGS proteins are important effectors of Ras- and Raf-mediated oncogenesis. We will determine if suppressing RGS protein expression will impair the ability of oncogenic H-Ras to promote growth transformation and tumorigenic growth of fibroblast and epithelial cells, and/or impair the transformed and tumorigenic growth of B-Raf


mutation positive melanoma and colorectal carcinoma cell lines. We will also employ fluorescence-based techniques to determine the dynamic relationship between H-Ras and RGS proteins in cells, as well as x-ray crystallographic techniques to delineate the precise nature of RGS protein domain associations with H-Ras, B-Raf and MEK2 to develop a better understanding of the mechanisms of RGS protein regulation of ERK signaling. Role: Co-investigator on one aim that is directed at x-ray protein crystallography of RGS protein domains. R03 DA030555-02 Siderovski (PI) 4/01/10 – 3/31/12 NIH/NIDA Enzymatic Screen for RGS Protein Modulators We entered a newly-developed enzymatic-based assay of RGS protein GTPase-accelerating activity into the NIH Roadmap’s Molecular Libraries Probe Production Center Network (MLPCN), as well as supported the MLPCN screening effort by analyzing hit compounds with secondary assays that employ orthogonal techniques. Role: PD/PI. R01 GM074268 Siderovski (PI) 7/1/06 – 6/30/11 NIH/NIGMS Mechanistic Studies of a Novel G-alpha Nucleotide Cycle The major goals of this project are to (a) to define the structural determinants and functional interplay between novel Ga regulators (including RIC-8, RGS-7, and GPR-1/-2) of the model organism Caenorhabditis elegans that control GOA-1 and GPA-16 Ga subunit activity in the process of asymmetric cell division, (b) develop new peptide-based fluorescence biosensors to assess the spatiotemporal dynamics of Ga nucleotide state in live cells during cell division, and (c) to define the structural features and combined biochemical actions of mammalian Gai proteins, essential regulators of their nucleotide cycle, and the cell-cycle kinase Cdk1 in modulating microtubule dynamics during mitosis. Role: PI. R01 GM082892-03S1 Siderovski (PI) NIH/NIGMS $39,657 for one-time equipment purchase ARRA Supplement – Structural Determinants of Heterotrimeric G-protein Nucleotide Cycling To accelerate the pace of research under the parent R01 grant, we received funds for a Berthold Mithras LB 940 microplate reader that will enable use of a novel BRET-based readout of GPCR/heterotrimer activation. Role: PD/PI. R01 GM062338 Siderovski (PI) 2/1/01 – 1/31/11 NIH/NIGMS G-protein Signal Coordination by RGS12 The major goals of this study are to define the specific roles that RGS12 partakes in ion channel modulation in dorsal root ganglion neurons and thus illuminate the potential for RGS12 as a drug discovery target for novel therapies for neuropathic pain and spasticity. This project involves biochemical/biophysical and cell-biological analyses of RGS12-mediated protein/protein and protein/lipid interactions with signal transduction components downstream of the GABA(B)-receptor, coupled with electrophysiological assessment of neurotransmitter modulation of Cav2.2 calcium channel activity in the presence of selective RGS12 loss-of-function mutants. Role: PI.


R03 NS053754-01 Siderovski (PI) 9/30/05 – 8/31/09 NIH/NINDS Real-time Fluorescence Assays of RGS Domain GAP Activity The major goal of this study was to modify and validate one of three novel, real-time, fluorescence-based assay of RGS protein function for automated high-throughput molecular screening. $25,000 direct cost supplements (3 R03 NS053754-01S1/S2) have been awarded by the NIH Roadmap’s Neuroscience Blueprint for delivering a high-throughput screen to one of the Roadmap’s screening centers, in support of follow-up secondary and counter-screening efforts. Innovation Award Siderovski (PI) 2/01/2008 – 6/30/2009 UNC/UCRF Genetically-engineered mouse model studies of RGS12 We recently determined that the “regulator of G protein signaling” (RGS) protein RGS12, best known for regulating heterotrimeric G protein signaling, is also a putative effector of the small GTPases H-Ras and N-Ras; in addition, RGS12 may function as a scaffold protein that regulates a key Ras effector pathway: the Raf-MEK-ERK cascade. In light of the important role of the ERK MAPK pathway in neoplastic cell biology, we hypothesize that RGS12 is an key effector of Ras- and/or Raf-mediated oncogenesis. RGS12 is also seen to acquire somatic mutations in human colorectal cancer samples with high microsatellite instability. We wish to test whether RGS12 plays an important role as an effector of Ras- and Raf-mediated transformation in an organismal context of in vivo tumor development. Initial UCRF investment will allow us to generate a conditional Rgs12-deficient mouse and begin to test the role of RGS12 in skin papilloma and colorectal cancer development, as well as in melanoma development, thereby establishing preliminary findings for future R01 and postdoctoral fellowship grant applications. Role: PI. P01 GM065533 Harden (PI) 4/10/2002 – 3/31/2008 NIH/NIGMS G-protein Signal Integration by Multifunctional Proteins The long-term goal was to elucidate mechanistic and structural details underlying the involvement of RGS proteins and PLCepsilon in coordinating heterotrimeric and Ras-family G protein signaling. Dr. Siderovski was a co-investigator (Dr. Harden was Principal Investigator) on Project I (“R7 RGS protein-mediated regulation of GPCR signaling”), a co-investigator (Dr. J. Sondek was Principal Investigator) on Project IV (“Structures of novel R7 and R12 protein domains”), and co-director (with Dr. Sondek) of the Protein Core, which provided rapid automated purification and functional analyses of proteins that impinge on G-protein signaling. New Investigator Award Siderovski (PI) 7/01/2001 – 6/30/2004 Burroughs Wellcome Fund GoLoco motif-derived peptides as selective G-protein “perturbagens” The major goal of this project was to test the hypothesis that the GoLoco motifs of RGS proteins can be developed into cell membrane-permeant peptides to enable intracellular delivery of guanine-nucleotide dissociation inhibitor (GDI) activity directed toward select Ga subunits. Role: PI Scholar Research Program Siderovski (PI) 1/01/2001 – 12/31/2003 The EJLB Foundation Pharmacological studies of RGS2 induction and function in dopaminergic circuitry The major goal was to test whether RGS2 induction in the mouse CNS upon dopaminergic stimuli would affect neurotransmitter signaling via receptor attenuation. Role: PI


Sponsored Research Siderovski (PI) 7/01/2002 – 6/30/2004 Karo*Bio USA A Structural Determination of Peptide Interaction with G-alpha Proteins This industrially-sponsored research program was focused on characterizing the structural interactions of selected phage-display peptides with G-alpha proteins using X-ray crystallography and determining the effects of these peptides on G-alpha function. Role: PI Sponsored Research Siderovski (PI) 4/01/2001 – 3/31/2003 INSPIRE Pharmaceuticals Anti-RGS Activity High-throughput Assay Development This industrially-sponsored research program was focused on derivatization of RGS protein assays (G-alpha binding and G-alpha GTPase activity) for non-radioactive, high-throughput screening of chemical libraries for anti-RGS activity. Role: PI

Multi-User Equipment Grant Siderovski (PI) 12/2001 North Carolina Biotechnology Center Multi-User Surface Plasmon Resonance Biosensor System Institutional development grant-in-aid for the purchase of a $300,000 BIAcore 3000 surface plasmon resonance biosensor analyzer of protein-protein, protein-lipid, and protein-drug interactions. Role: Program Director


Bibliography of David P. Siderovski

Books and book chapters -

10. Van Dyke K, Siderovski DP. Chapter 39 - Drugs for Gout. In: Fink, Leah & Woodfork, Karen, editors. Illustrated Pharmacology, 7th Edition. Lippincott Williams & Wilkins; [in press].

9. Siderovski DP, Unger K. Chapter 19 - Anti-hyperlipidemic Drugs and Coronary Artery Disease. In: Fink, Leah & Woodfork, Karen, editors. Illustrated Pharmacology, 7th Edition. Lippincott Williams & Wilkins; [in press].

8. Kimple AJ, Yasgar A, Hughes M, Jadhav A, Willard FS, Muller RE, Austin CP, Inglese J, Ibeanu GC, Siderovski DP, Simeonov A. A Homogeneous Platform to Discover Inhibitors of the GoLoco Motif/Ga Interaction. In: Chaguturu, Rathnam, editor. Advances in Combinatorial Chemistry & High Throughput Screening. Bentham Science; 2013.

7. Johnston CA, Willard FS, Ramer K, Blaesius R, Roques N, Siderovski DP. G-Protein Activation State-Selective Binding Peptides as New Tools for Probing Heterotrimeric G-protein Subunit Signaling Dynamics. In: Chaguturu, Rathnam, editor. Advances in Combinatorial Chemistry & High Throughput Screening. Bentham Science; 2013.

6. Siderovski DP, Kimple AJ. Regulator of G-protein Signaling (RGS) Protein Family. In: Choi, Sangdun, editor. The Encyclopedia of Signaling Molecules. 1st ed. New York (NY): Springer; 2013, XLVIII, 2030 pp.

5. Siderovski DP, Kimple AJ, Willard FS. Large G-proteins. In: Begley TP, editor. Wiley Encyclopedia of Chemical Biology. 1st ed. Hoboken (NJ): John Wiley & Sons; 2009.

4. Willard MD, Willard FS, Siderovski DP. The superfamily of ‘regulator of G-protein signaling’ (RGS) proteins. In: Bradshaw RA, Dennis EA, editors. Handbook of Cell Signaling. 2nd ed. San Diego (CA): Elsevier Press; 2009.

3. Siderovski DP, editor. Methods in Enzymology volume 390: Regulators of G-protein signaling, part B. San Diego (CA): Academic Press; 2004. 434 pp.

2. Siderovski DP, editor. Methods in Enzymology volume 389: Regulators of G-protein signaling, part A. San Diego (CA): Academic Press; 2004. 516 pp.

1. Siderovski DP, Harden TK. The RGS protein superfamily. In: Bradshaw RA, Dennis EA, editors. Handbook of Cell Signaling. 1st ed. San Diego (CA): Elsevier Press; 2003. p 631-638.

Peer-reviewed primary research articles -

120. Schroer AB, Gross JD, Kaski SW, Wix KA, Siderovski DP, Vandenbeuch A, Setola V. Development of full sweet, umami, and bitter taste responsiveness requires Regulator of G protein Signaling-21 (RGS21). Chemical Senses 2018; 43(5):367-378.

119. Gross JD, Kaski SW, Schroer AB, Wix KA, Siderovski DP, Setola V. Regulator of G

protein Signaling-12 (RGS12) modulates the dopamine transporter in ventral striatum and locomotor responses to psychostimulants. J Psychopharmacology 2018; 32(2):191-203.


118. George T, Bell M, Chakraborty M, Siderovski DP, Giembycz MA, Newton R. Protective roles for RGS2 in a mouse model of house dust mite-induced airway inflammation. PLoS One 2017; 12(1): e0170269.

117. Gall BJ, Schroer AB, Gross JD, Setola V, Siderovski DP. Reduction of GPSM3 expression akin to the arthritis-protective SNP rs204989 differentially affects migration in a neutrophil model. Genes Immun 2016; 17(6):321-7.

116. Gall BJ, Wilson A, Schroer AB, Gross JD, Stoilov P, Setola V, Watkins CM, Siderovski DP. Genetic variations in GPSM3 associated with protection from rheumatoid arthritis affect its transcript abundance. Genes Immun 2016; 17(2):139-147.

115. Ma P, Ou K, Sinnamon AJ, Jiang H, Siderovski DP, Brass LF. Modulating platelet reactivity through control of RGS18 availability. Blood. 2015; 126(24):2611-2620.

114. Zha Z, Han X, Smith MD, Liu Y, Giguère PM, Kopanja D, Raychaudhuri P, Siderovski DP, Guan KL, Lei QY, Xiong Y. A Non-Canonical Function of Gbeta as a Subunit of E3 Ligase Targeting GRK2 Ubiquitylation. Mol. Cell 2015; 58(5):794-803.

113. Bosch DE, Siderovski DP. Entamoeba histolytica RacC Selectively Engages p21-Activated Kinase Effectors. Biochemistry. 2015; 54(2):404-12.

112. Guipponi M, Santoni FA, Setola V, Gehrig C, Rotharmel M, Cuenca M, Guillin O, Dikeos D, Georgantopoulos G, Papadimitriou G, Curtis L, Méary A, Schürhoff F, Jamain S, Avramopoulos D, Leboyer M, Rujescu D, Pulver A, Campion D, Siderovski DP, Antonarakis SE. Exome sequencing in 53 sporadic cases of schizophrenia identifies 18 putative candidate genes. PLoS One. 2014; 9(11):e112745.

111. Giguère PM, Gall BJ, Ezekwe EA Jr, Laroche G, Buckley BK, Kebaier C, Wilson JE, Ting JP, Siderovski DP, Duncan JA. G protein Signaling Modulator-3 inhibits the inflammasome activity of NLRP3. J Biol Chem. 2014; 289(48):33245-57.

110. Chen B, Siderovski DP, Neubig RR, Lawson MA, Trejo J. Regulation of protease-activated receptor 1 signaling by the adaptor protein complex 2 and R4 subfamily of regulator of G protein signaling proteins. J Biol Chem. 2014; 289(3):1580-91.

109. Holden NS, George T, Rider CF, Chandrasekhar A, Shah S, Kaur M, Johnson M, Siderovski DP, Leigh R, Giembycz MA, Newton R. Induction of RGS2 expression by long-acting β2-adrenoceptor agonists and glucocorticoids in human airway epithelial cells. J Pharmacol Exp Ther. 2014; 348(1):12-24.

108. Kimple AJ, Garland A, Cohen SP, Setola V, Willard FS, Zielinski T, Lowery RG, Tarran R, Siderovski DP. RGS21, a regulator of taste and mucociliary clearance? Laryngoscope 2014; 124(3):E56-63.

107. Tarrant TK, Billard MJ, Timoshchenko RG, McGinnis MW, Serafin DS, Foreman O, Esserman DA, Chao NJ, Lento WE, Lee DM, Patel D, Siderovski DP. G protein-coupled receptor kinase-3-deficient mice exhibit WHIM syndrome features and attenuated inflammatory responses. J Leukoc Biol. 2013; 94(6):1243-51.

106. Garcia-Olivares J, Torres-Salazar D, Owens WA, Baust T, Siderovski DP, Amara SG, Zhu J, Daws LC, Torres GE. Inhibition of dopamine transporter activity by G protein {beta}{gamma} subunits. PLoS One 2013; 8(3):e59788.


105. Giguère PM, Billard MJ, Laroche G, Buckley BK, Timoshchenko RG, McGinnis MW, Esserman D, Foreman O, Liu P, Siderovski DP, Tarrant TK. G-protein signaling modulator-3, a gene linked to autoimmune diseases, regulates monocyte function and its deficiency protects from inflammatory arthritis. Mol Immunol. 2013; 54(2):193-8.

104. Bosch DE, Kimple AJ, Manning AJ, Muller RE, Willard FS, Machius M, Rogers SL,

Siderovski DP. Structural Determinants of RGS-RhoGEF Signaling Critical to Entamoeba histolytica Pathogenesis. Structure. 2013; 21(1):65-75. PMID: 23260656.

103. Bosch DE, Siderovski DP. Structural determinants of ubiquitin conjugation in Entamoeba

histolytica. J Biol Chem. 2013; 288(4):2290-302. PMID: 23209297. 102. Bosch DE, Kimple AJ, Muller RE, Giguère PM, Machius M, Willard FS, Temple BR,

Siderovski DP. Heterotrimeric G-protein signaling is critical to pathogenic processes in Entamoeba histolytica. PLoS Pathog. 2012; 8(11):e1003040.

101. Cohen SP, Buckley BK, Kosloff M, Garland AL, Bosch DE, Cheng JG, Radhakrishna H,

Brown MD, Willard FS, Arshavsky VY, Tarran R, Siderovski DP, Kimple AJ. Regulator of G-protein Signaling-21 (RGS21) is an inhibitor of bitter gustatory signaling found in lingual and airway epithelia. J Biol Chem. 2012; 287(50):41706-19.

100. Bosch DE, Yang B, Siderovski DP. Entamoeba histolytica Rho1 regulates actin

polymerization through a divergent, Diaphanous-related formin. Biochemistry 2012; 51(44):8791-801.

99. Giguère PM, Laroche G, Oestreich EA, Duncan JA, Siderovski DP. Regulation of the

Subcellular Localization of the G-protein Subunit Regulator GPSM3 through Direct Association with 14-3-3 Protein. J Biol Chem. 2012; 287(37):31270-9.

98. Lei Y, Wen H, Yu Y, Taxman DJ, Zhang L, Widman DG, Swanson KV, Wen KW,

Damania B, Moore CB, Giguere PM, Siderovski DP, Hiscott J, Razani B, Semenkovich CF, Chen X, Ting JP. The mitochondrial proteins NLRX1 and TUFM form a complex that regulates type 1 interferon and autophagy. Immunity 2012; 36:933-46.

97. Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP.

A P-loop mutation in Galpha subunits prevents transition to the active state: Implications for G-protein signaling in fungal pathogenesis. PLoS Pathog. 2012; 8(2):e1002553.

96. Giguère PM, Laroche G, Oestreich EA, Siderovski DP. GPSM3 regulates heterotrimeric

G protein dynamics through a dual association with Gbeta and Galpha-i subunits. J Biol Chem. 2012; 287(7):4863-74.

95. Holden NS, Bell MJ, Rider CF, King EM, Gaunt DD, Leigh R, Johnson M, Siderovski DP,

Heximer SP, Giembycz MA, Newton R. Proc Natl Acad Sci U S A. 2011; 108(49):19713-8 94. Bosch DE, Wittchen ES, Qiu C, Burridge K, Siderovski DP. Unique structural and

nucleotide exchange features of the Rho1 GTPase of Entamoeba histolytica. J Biol Chem. 2011; 286(45):39236-46.


93. Kosloff M, Travis AM, Bosch DE, Siderovski DP, Arshavsky VY. Integrating energy calculations with functional assays to decipher the specificity of G protein-RGS protein interactions. Nat Struct Mol Biol. 2011; 18(7):846-53.

92. Sammond DW, Bosch DE, Butterfoss GL, Purbeck C, Machius M, Siderovski DP, Kuhlman B. Computational design of the sequence and structure of a protein-binding peptide. J Am Chem Soc. 2011; 133(12):4190-2.

91. Bosch DE, Kimple AJ, Sammond DW, Muller RE, Miley MJ, Machius M, Kuhlman B, Willard FS, Siderovski DP. Structural determinants of affinity enhancement between GoLoco motifs and G-protein alpha subunit mutants. J Biol Chem. 2011; 286(5):3351-8

90. Muller RE, Klein KR, Hutsell SQ, Siderovski DP, Kimple AJ. A homogeneous method to measure nucleotide exchange by alpha-subunits of heterotrimeric G-proteins using fluorescence polarization. Assay Drug Dev Technol. 2010; 8(5):621-4.

89. Laroche G, Giguère PM, Roth BL, Trejo J, Siderovski DP. RNA interference screen for RGS protein specificity at muscarinic and protease-activated receptors reveals bidirectional modulation of signaling. Am J Physiol Cell Physiol. 2010; 299(3):C654-64.

88. Zheng Z, Zhu H, Wan Q, Liu J, Xiao Z, Siderovski DP, Du Q. LGN regulates mitotic spindle orientation during epithelial morphogenesis. J Cell Biol. 2010;189(2):275-88.

87. Lambert NA, Johnston CA, Cappell SD, Kuravi S, Kimple AJ, Willard FS, Siderovski DP. Regulators of G-protein signaling accelerate GPCR signaling kinetics and govern sensitivity solely by accelerating GTPase activity. Proc Natl Acad Sci U S A. 2010;107(15):7066-71.

86. Nakamura K, Kimple AJ, Siderovski DP, Johnson GL. PB1 domain interaction of p62/sequestosome 1 and MEKK3 regulates NF-kappaB activation. J Biol Chem. 2010;285(3):2077-89.

85. Zielinski T, Kimple AJ, Hutsell SQ, Koeff MD, Siderovski DP, Lowery RG. Two Galpha(i1) rate-modifying mutations act in concert to allow receptor-independent, steady-state measurements of RGS protein activity. J Biomol Screen. 2009;14(10):1195-206.

84. Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP. Structural determinants of G-protein alpha subunit selectivity by regulator of G-protein signaling 2 (RGS2). J Biol Chem. 2009;284(29):19402-11.

83. Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP. Structural determinants of G-protein alpha subunit selectivity by regulator of G-protein signaling 2 (RGS2). J Biol Chem. 2009;284(29):19402-11.

82. Willard FS, Willard MD, Kimple AJ, Soundararajan M, Oestreich EA, Li X, Sowa NA, Kimple RJ, Doyle DA, Der CJ, Zylka MJ, Snider WD, Siderovski DP. Regulator of G-protein signaling 14 (RGS14) is a selective H-Ras effector. PLoS One. 2009;4(3):e4884.

81. Preininger A, Funk M, Meier S, Oldham W, Johnston C, Adhikary S, Kimple A, Siderovski D, Hamm H, Iverson T. Helix dipole movement and conformational variability contribute to allosteric GDP release in Gi subunits. Biochemistry 2009;48(12):2630-42.


80. Takimoto E, Koitabashi N, Hsu S, Ketner EA, Zhang M, Nagayama T, Bedja D, Gabrielson KL, Blanton R, Siderovski DP, Mendelsohn ME, Kass DA. Regulator of G protein signaling 2 mediates cardiac compensation to pressure overload and antihypertrophic effects of PDE5 inhibition in mice. J Clin Invest 2009;119(2):408-20.

79. Willard FS, Zheng Z, Guo J, Digby GJ, Kimple AJ, Conley JM, Johnston CA, Bosch D, Willard MD, Watts VJ, Lambert NA, Ikeda SR, Du Q, Siderovski DP. A point mutation to G-alpha-i selectively blocks GoLoco motif binding: Direct evidence for G-alpha/GoLoco complexes in mitotic spindle dynamics. J Biol Chem 2008;283(52):36698-710.

78. Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP. Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits. Proc Natl Acad Sci U S A 2008;105(17):6457-62.

77. Johnston CA, Afshar K, Snyder JT, Tall GG, Gonczy P, Siderovski DP, Willard FS. Structural determinants underlying the temperature-sensitive nature of a Galpha mutant in C. elegans asymmetric cell division. J Biol Chem 2008;283(31):21550-8.

76. Kimple AJ, Yasgar A, Hughes M, Jadhav A, Willard FS, Muller RE, Austin CP, Inglese J, Ibeanu GC, Siderovski DP, Simeonov A. A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interaction. Comb Chem High Throughput Screen 2008;11(5)-396-409.

75. Cheever ML, Snyder JT, Gershburg S, Siderovski DP, Harden TK, Sondek J. Crystal structure of the multifunctional Gbeta5-RGS9 complex. Nat Struct Mol Biol 2008;15(2):155-62.

74. Liu H, Suresh A, Willard FS, Siderovski DP, Lu S, Naqvi NI. Rgs1 regulates multiple Galpha subunits in Magnaporthe pathogenesis, asexual growth and thigmotropism. Embo J 2007;26(3):690-700.

73. Willard FS, Low AB, McCudden CR, Siderovski DP. Differential G-alpha interaction capacities of the GoLoco motifs in Rap GTPase activating proteins. Cell Signal 2007;19(2):428-38.

72. Willard MD, Willard FS, Li X, Cappell SD, Snider WD, Siderovski DP. Selective role for RGS12 as a Ras/Raf/MEK scaffold in nerve growth factor-mediated differentiation. Embo J 2007;26(8):2029-40.

71. Sammond DW, Eletr ZM, Purbeck C, Kimple RJ, Siderovski DP, Kuhlman B. Structure-based protocol for identifying mutations that enhance protein-protein binding affinities. J Mol Biol 2007;371(5):1392-404.

70. Kimple AJ, Willard FS, Giguere PM, Johnston CA, Mocanu V, Siderovski DP. The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Galpha-interaction face. Biochim Biophys Acta 2007;1774(9):1213-20.

69. Johnston CA, Taylor JP, Gao Y, Kimple AJ, Grigston JC, Chen JG, Siderovski DP, Jones AM, Willard FS. GTPase acceleration as the rate-limiting step in Arabidopsis G protein-coupled sugar signaling. Proc Natl Acad Sci U S A 2007;104(44):17317-22.


68. Sambi BS, Hains MD, Waters CM, Connell MC, Willard FS, Kimple AJ, Pyne S, Siderovski DP, Pyne NJ. The effect of RGS12 on PDGFbeta receptor signalling to p42/p44 mitogen activated protein kinase in mammalian cells. Cell Signal 2006;18(7):971-81.

67. Willard FS, McCudden CR, Siderovski DP. G-protein alpha subunit interaction and guanine nucleotide dissociation inhibitor activity of the dual GoLoco motif protein PCP-2 (Purkinje cell protein-2). Cell Signal 2006;18(8):1226-34.

66. Willard FS, Siderovski DP. The R6A-1 peptide binds to switch II of Gai1 but is not a GDP-dissociation inhibitor. Biochem Biophys Res Commun 2006;339(4):1107-12.

65. Fatemi SH, Reutiman TJ, Folsom TD, Bell C, Nos L, Fried P, Pearce DA, Singh S,

Siderovski DP, Willard FS, Fukuda M. Chronic olanzapine treatment causes differential expression of genes in frontal cortex of rats as revealed by DNA microarray technique. Neuropsychopharmacology 2006;31(9):1888-99.

64. Chasse SA, Flanary P, Parnell SC, Hao N, Cha JY, Siderovski DP, Dohlman HG. Genome-scale analysis reveals Sst2 as the principal regulator of mating pheromone signaling in the yeast Saccharomyces cerevisiae. Eukaryot Cell 2006;5(2):330-46.

63. Hains MD, Wing MR, Maddileti S, Siderovski DP, Harden TK. Galpha12/13- and rho-dependent activation of phospholipase C-epsilon by lysophosphatidic acid and thrombin receptors. Mol Pharmacol 2006;69(6):2068-75.

62. Paing MM, Johnston CA, Siderovski DP, Trejo J. Clathrin adaptor AP2 regulates thrombin receptor constitutive internalization and endothelial cell resensitization. Mol Cell Biol 2006;26(8):3231-42.

61. Willard FS, Siderovski DP. Covalent immobilization of histidine-tagged proteins for surface plasmon resonance. Anal Biochem 2006;353(1):147-9.

60. Dho SE, Trejo J, Siderovski DP, McGlade CJ. Dynamic regulation of mammalian numb by G protein-coupled receptors and protein kinase C activation: Structural determinants of numb association with the cortical membrane. Mol Biol Cell 2006;17(9):4142-55.

59. Johnston CA, Lobanova ES, Shavkunov AS, Low J, Ramer JK, Blaesius R, Fredericks Z, Willard FS, Kuhlman B, Arshavsky VY, Siderovski DP. Minimal determinants for binding activated G alpha from the structure of a G alpha(i1)-peptide dimer. Biochemistry 2006;45(38):11390-400.

58. Richman RW, Strock J, Hains MD, Cabanilla NJ, Lau KK, Siderovski DP, Diverse-Pierluissi M. RGS12 interacts with the SNARE-binding region of the Cav2.2 calcium channel. J Biol Chem 2005;280(2):1521-8.

57. Webb CK, McCudden CR, Willard FS, Kimple RJ, Siderovski DP, Oxford GS. D2 dopamine receptor activation of potassium channels is selectively decoupled by Galpha-specific GoLoco motif peptides. J Neurochem 2005;92(6):1408-18.

56. Willard FS, Kimple AJ, Johnston CA, Siderovski DP. A direct fluorescence-based assay for RGS domain GTPase accelerating activity. Anal Biochem 2005;340(2):341-51.

55. Martin-McCaffrey L, Willard FS, Pajak A, Dagnino L, Siderovski DP, D'Souza SJ. RGS14 is a microtubule-associated protein. Cell Cycle 2005;4(7):953-60.


54. McCudden CR, Willard FS, Kimple RJ, Johnston CA, Hains MD, Jones MB, Siderovski DP. G alpha selectivity and inhibitor function of the multiple GoLoco motif protein GPSM2/LGN. Biochim Biophys Acta 2005;1745(2):254-64.

53. Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP. Structure of Galpha(i1) bound to a GDP-selective peptide provides insight into guanine nucleotide exchange. Structure 2005;13(7):1069-80.

52. Martin-McCaffrey L, Hains MD, Pritchard GA, Pajak A, Dagnino L, Siderovski DP, D'Souza SJ. Differential expression of regulator of G-protein signaling R12 subfamily members during mouse development. Dev Dyn 2005;234(2):438-44.

51. Afshar K, Willard FS, Colombo K, Siderovski DP, Gonczy P. Cortical localization of the Galpha protein GPA-16 requires RIC-8 function during C. elegans asymmetric cell division. Development 2005;132(20):4449-59.

50. Johnston CA, Ramer JK, Blaesius R, Fredericks Z, Watts VJ, Siderovski DP. A bifunctional Galphai/Galphas modulatory peptide that attenuates adenylyl cyclase activity. FEBS Lett 2005;579(25):5746-50.

49. Wang H, Ng KH, Qian H, Siderovski DP, Chia W, Yu F. Ric-8 controls Drosophila neural progenitor asymmetric division by regulating heterotrimeric G proteins. Nat Cell Biol 2005;7(11):1091-8.

48. Zigman M, Cayouette M, Charalambous C, Schleiffer A, Hoeller O, Dunican D, McCudden CR, Firnberg N, Barres BA, Siderovski DP, Knoblich JA. Mammalian inscuteable regulates spindle orientation and cell fate in the developing retina. Neuron 2005;48(4):539-45.

47. Kimple RJ, Willard FS, Hains MD, Jones MB, Nweke GK, Siderovski DP. Guanine nucleotide dissociation inhibitor activity of the triple GoLoco motif protein G18: alanine-to-aspartate mutation restores function to an inactive second GoLoco motif. Biochem J 2004;378(Pt 3):801-8.

46. Afshar K, Willard FS, Colombo K, Johnston CA, McCudden CR, Siderovski DP, Gonczy P. RIC-8 is required for GPR-1/2-dependent Galpha function during asymmetric division of C. elegans embryos. Cell 2004;119(2):219-30.

45. Martin-McCaffrey L, Willard FS, Oliveira-dos-Santos AJ, Natale DR, Snow BE, Kimple RJ, Pajak A, Watson AJ, Dagnino L, Penninger JM, Siderovski DP, D'Souza SJ. RGS14 is a mitotic spindle protein essential from the first division of the mammalian zygote. Dev Cell 2004;7(5):763-9.

44. Pruitt WM, Karnoub AE, Rakauskas AC, Guipponi M, Antonarakis SE, Kurakin A, Kay BK, Sondek J, Siderovski DP, Der CJ. Role of the pleckstrin homology domain in intersectin-L Dbl homology domain activation of Cdc42 and signaling. Biochim Biophys Acta 2003;1640(1):61-8.

43. Colombo K, Grill SW, Kimple RJ, Willard FS, Siderovski DP, Gonczy P. Translation of polarity cues into asymmetric spindle positioning in Caenorhabditis elegans embryos. Science 2003;300(5627):1957-61.


42. Chen JG, Willard FS, Huang J, Liang J, Chasse SA, Jones AM, Siderovski DP. A seven-transmembrane RGS protein that modulates plant cell proliferation. Science 2003;301(5640):1728-31.

41. Tang KM, Wang GR, Lu P, Karas RH, Aronovitz M, Heximer SP, Kaltenbronn KM, Blumer KJ, Siderovski DP, Zhu Y, Mendelsohn ME. Regulator of G-protein signaling-2 mediates vascular smooth muscle relaxation and blood pressure. Nat Med 2003;9(12):1506-12.

40. Rossman KL, Worthylake DK, Snyder JT, Siderovski DP, Campbell SL, Sondek J. A crystallographic view of interactions between Dbs and Cdc42: PH domain-assisted guanine nucleotide exchange. Embo J 2002;21(6):1315-26.

39. Kimple RJ, Kimple ME, Betts L, Sondek J, Siderovski DP. Structural determinants for GoLoco-induced inhibition of nucleotide release by Galpha subunits. Nature 2002;416(6883):878-81.

38. Wang Q, Liu M, Mullah B, Siderovski DP, Neubig RR. Receptor-selective effects of endogenous RGS3 and RGS5 to regulate mitogen-activated protein kinase activation in rat vascular smooth muscle cells. J Biol Chem 2002;277(28):24949-58.

37. Snyder JT, Worthylake DK, Rossman KL, Betts L, Pruitt WM, Siderovski DP, Der CJ, Sondek J. Structural basis for the selective activation of Rho GTPases by Dbl exchange factors. Nat Struct Biol 2002;9(6):468-75.

36. Booden MA, Siderovski DP, Der CJ. Leukemia-associated Rho guanine nucleotide exchange factor promotes G alpha q-coupled activation of RhoA. Mol Cell Biol 2002;22(12):4053-61.

35. Lambert JM, Lambert QT, Reuther GW, Malliri A, Siderovski DP, Sondek J, Collard JG, Der CJ. Tiam1 mediates Ras activation of Rac by a PI(3)K-independent mechanism. Nat Cell Biol 2002;4(8):621-5.

34. Evanko DS, Thiyagarajan MM, Siderovski DP, Wedegaertner PB. Gbeta gamma isoforms selectively rescue plasma membrane localization and palmitoylation of mutant Galphas and Galphaq. J Biol Chem 2001;276(26):23945-53.

33. Kimple RJ, De Vries L, Tronchere H, Behe CI, Morris RA, Gist Farquhar M, Siderovski DP. RGS12 and RGS14 GoLoco motifs are G alpha(i) interaction sites with guanine nucleotide dissociation inhibitor activity. J Biol Chem 2001;276(31):29275-81.

32. Kimple ME, Siderovski DP, Sondek J. Functional relevance of the disulfide-linked complex of the N-terminal PDZ domain of InaD with NorpA. Embo J 2001;20(16):4414-22.

31. Snyder JT, Rossman KL, Baumeister MA, Pruitt WM, Siderovski DP, Der CJ, Lemmon MA, Sondek J. Quantitative analysis of the effect of phosphoinositide interactions on the function of Dbl family proteins. J Biol Chem 2001;276(49):45868-75.

30. Wing MR, Houston D, Kelley GG, Der CJ, Siderovski DP, Harden TK. Activation of phospholipase C-epsilon by heterotrimeric G protein betagamma-subunits. J Biol Chem 2001;276(51):48257-61.


29. Blake BL, Wing MR, Zhou JY, Lei Q, Hillmann JR, Behe CI, Morris RA, Harden TK, Bayliss DA, Miller RJ, Siderovski DP. G beta association and effector interaction selectivities of the divergent G gamma subunit G gamma(13). J Biol Chem 2001;276(52):49267-74.

28. Bessant DA, Payne AM, Snow BE, Antino G, Mehdi SQ, Bird AC, Siderovski DP, Bhattacharya SS. Importance of the autosomal recessive retinitis pigmentosa locus on 1q31-q32.1 (RP12) and mutation analysis of the candidate gene RGS16 (RGS-r). J Med Genet 2000;37(5):384-7.

27. Zhou JY, Siderovski DP, Miller RJ. Selective regulation of N-type Ca channels by different combinations of G-protein beta/gamma subunits and RGS proteins. J Neurosci 2000;20(19):7143-8.

26. Liu Y, Snow BE, Hande MP, Baerlocher G, Kickhoefer VA, Yeung D, Wakeham A, Itie A, Siderovski DP, Lansdorp PM, Robinson MO, Harrington L. Telomerase-associated protein TEP1 is not essential for telomerase activity or telomere length maintenance in vivo. Mol Cell Biol 2000;20(21):8178-84.

25. Oliveira-Dos-Santos AJ, Matsumoto G, Snow BE, Bai D, Houston FP, Whishaw IQ, Mariathasan S, Sasaki T, Wakeham A, Ohashi PS, Roder JC, Barnes CA, Siderovski DP, Penninger JM. Regulation of T cell activation, anxiety, and male aggression by RGS2. Proc Natl Acad Sci U S A 2000;97(22):12272-7.

24. Liu Y, Snow BE, Hande MP, Yeung D, Erdmann NJ, Wakeham A, Itie A, Siderovski DP, Lansdorp PM, Robinson MO, Harrington L. The telomerase reverse transcriptase is limiting and necessary for telomerase function in vivo. Curr Biol 2000;10(22):1459-62.

23. De Vries L, Fischer T, Tronchere H, Brothers GM, Strockbine B, Siderovski DP, Farquhar MG. Activator of G protein signaling 3 is a guanine dissociation inhibitor for Galpha i subunits. Proc Natl Acad Sci U S A 2000;97(26):14364-9.

22. Schiff ML, Siderovski DP, Jordan JD, Brothers G, Snow B, De Vries L, Ortiz DF, Diverse-Pierluissi M. Tyrosine-kinase-dependent recruitment of RGS12 to the N-type calcium channel. Nature 2000;408(6813):723-7.

21. Susin SA, Lorenzo HK, Zamzami N, Marzo I, Snow BE, Brothers GM, Mangion J, Jacotot E, Costantini P, Loeffler M, Larochette N, Goodlett DR, Aebersold R, Siderovski DP, Penninger JM, Kroemer G. Molecular characterization of mitochondrial apoptosis-inducing factor. Nature 1999;397(6718):441-6.

20. Snow BE, Betts L, Mangion J, Sondek J, Siderovski DP. Fidelity of G protein beta-subunit association by the G protein gamma-subunit-like domains of RGS6, RGS7, and RGS11. Proc Natl Acad Sci U S A 1999;96(11):6489-94.

19. Snow BE, Antonio L, Suggs S, Siderovski DP. Cloning of a retinally abundant regulator of G-protein signaling (RGS-r/RGS16): genomic structure and chromosomal localization of the human gene. Gene 1998;206(2):247-53.

18. Yee AA, Yin P, Siderovski DP, Mak TW, Litchfield DW, Arrowsmith CH. Cooperative interaction between the DNA-binding domains of PU.1 and IRF4. J Mol Biol 1998;279(5):1075-83.


17. Snow BE, Hall RA, Krumins AM, Brothers GM, Bouchard D, Brothers CA, Chung S, Mangion J, Gilman AG, Lefkowitz RJ, Siderovski DP. GTPase activating specificity of RGS12 and binding specificity of an alternatively spliced PDZ (PSD-95/Dlg/ZO-1) domain. J Biol Chem 1998;273(28):17749-55.

16. Ingi T, Krumins AM, Chidiac P, Brothers GM, Chung S, Snow BE, Barnes CA, Lanahan AA, Siderovski DP, Ross EM, Gilman AG, Worley PF. Dynamic regulation of RGS2 suggests a novel mechanism in G-protein signaling and neuronal plasticity. J Neurosci 1998;18(18):7178-88.

15. Stambolic V, Suzuki A, de la Pompa JL, Brothers GM, Mirtsos C, Sasaki T, Ruland J, Penninger JM, Siderovski DP, Mak TW. Negative regulation of PKB/Akt-dependent cell survival by the tumor suppressor PTEN. Cell 1998;95(1):29-39.

14. Snow BE, Krumins AM, Brothers GM, Lee SF, Wall MA, Chung S, Mangion J, Arya S, Gilman AG, Siderovski DP. A G protein gamma subunit-like domain shared between RGS11 and other RGS proteins specifies binding to Gbeta5 subunits. Proc Natl Acad Sci U S A 1998;95(22):13307-12.

13. Snow BE, Antonio L, Suggs S, Gutstein HB, Siderovski DP. Molecular cloning and expression analysis of rat Rgs12 and Rgs14. Biochem Biophys Res Commun 1997;233(3):770-7.

12. McCracken S, Fong N, Rosonina E, Yankulov K, Brothers G, Siderovski D, Hessel A, Foster S, Shuman S, Bentley DL. 5'-Capping enzymes are targeted to pre-mRNA by binding to the phosphorylated carboxy-terminal domain of RNA polymerase II. Genes Dev 1997;11(24):3306-18.

11. Siderovski DP, Hessel A, Chung S, Mak TW, Tyers M. A new family of regulators of G-protein-coupled receptors? Curr Biol 1996;6(2):211-2.

10. Wu HK, Heng HH, Siderovski DP, Dong WF, Okuno Y, Shi XM, Tsui LC, Minden MD. Identification of a human LIM-Hox gene, hLH-2, aberrantly expressed in chronic myelogenous leukaemia and located on 9q33-34.1. Oncogene 1996;12(6):1205-12.

9. Grossman A, Mittrucker HW, Nicholl J, Suzuki A, Chung S, Antonio L, Suggs S, Sutherland GR, Siderovski DP, Mak TW. Cloning of human lymphocyte-specific interferon regulatory factor (hLSIRF/hIRF4) and mapping of the gene to 6p23-p25. Genomics 1996;37(2):229-33.

8. Matsuyama T, Grossman A, Mittrucker HW, Siderovski DP, Kiefer F, Kawakami T, Richardson CD, Taniguchi T, Yoshinaga SK, Mak TW. Molecular cloning of LSIRF, a lymphoid-specific member of the interferon regulatory factor family that binds the interferon-stimulated response element (ISRE). Nucleic Acids Res 1995;23(12):2127-36.

7. Wu HK, Heng HH, Shi XM, Forsdyke DR, Tsui LC, Mak TW, Minden MD, Siderovski DP. Differential expression of a basic helix-loop-helix phosphoprotein gene, G0S8, in acute leukemia and localization to human chromosome 1q31. Leukemia 1995;9(8):1291-8.

6. McMillan NA, Chun RF, Siderovski DP, Galabru J, Toone WM, Samuel CE, Mak TW, Hovanessian AG, Jeang KT, Williams BR. HIV-1 Tat directly interacts with the interferon-induced, double-stranded RNA-dependent kinase, PKR. Virology 1995;213(2):413-24.


5. Siderovski DP, Heximer SP, Forsdyke DR. A human gene encoding a putative basic helix-loop-helix phosphoprotein whose mRNA increases rapidly in cycloheximide-treated blood mononuclear cells. DNA Cell Biol 1994;13(2):125-47.

4. Siderovski DP, Mak TW. RAMHA: a PC-based Monte-Carlo simulation of random saturation mutagenesis. Comput Biol Med 1993;23(6):463-74.

3. Molina TJ, Kishihara K, Siderovski DP, van Ewijk W, Narendran A, Timms E, Wakeham A, Paige CJ, Hartmann KU, Veillette A, et al. Profound block in thymocyte development in mice lacking p56lck. Nature 1992;357(6374):161-4.

2. Siderovski DP, Matsuyama T, Frigerio E, Chui S, Min X, Erfle H, Sumner-Smith M, Barnett RW, Mak TW. Random mutagenesis of the human immunodeficiency virus type-1 trans-activator of transcription (HIV-1 Tat). Nucleic Acids Res 1992;20(20):5311-20.

1. Siderovski DP, Blum S, Forsdyke RE, Forsdyke DR. A set of human putative lymphocyte G0/G1 switch genes includes genes homologous to rodent cytokine and zinc finger protein-encoding genes. DNA Cell Biol 1990;9(8):579-87.

Review articles, Editorials, Letters -

29. Billard MJ, Gall BJ, Richards KL, Siderovski DP, Tarrant TK. G protein signaling modulator-3: a leukocyte regulator of inflammation in health and disease. Am J Clin Exp Immunol. 2014; 3(2):97-106.

28. Bosch DE, Siderovski DP. G protein signaling in the parasite Entamoeba histolytica. Exp Mol Med. 2013; 45:e15.

27. Bosch DE, Zielinski T, Lowery RG, Siderovski DP. Evaluating Modulators of “Regulator of G-protein Signaling” (RGS) Proteins. Curr Protoc Pharmacol. 2012; Ch. 2: Unit 2.8.

26. Kimple AJ, Bosch DE, Giguere PM, Siderovski DP. RGS proteins and their G-alpha substrates: Promises and challenges in their use as drug discovery targets. Pharm Rev. 2011; 63(3):728-49.

25. Kimple AJ, Muller RE, Siderovski DP, Willard FS. A capture coupling method for the covalent immobilization of hexahistidine tagged proteins for surface plasmon resonance. Methods Mol Biol. 2010;627:91-100.

24. Hutsell SQ, Kimple RJ, Siderovski DP, Willard FS, Kimple AJ. High-affinity immobilization of proteins using biotin- and GST-based coupling strategies. Methods Mol Biol. 2010;627:75-90.

23. Johnston CA, Willard MD, Kimple AJ, Siderovski DP, Willard FS. A sweet cycle for Arabidopsis G-proteins: Recent discoveries and controversies in plant G-protein signal transduction. Plant Signal Behav. 2008;3(12):1067-76.

22. Johnston CA, Willard FS, Ramer JK, Blaesius R, Roques CN, Siderovski DP. State-selective binding peptides for heterotrimeric G-protein subunits. Comb Chem High Throughput Screen 2008;11(5)370-81.

21. Johnston CA, Siderovski DP. Receptor-mediated activation of heterotrimeric G-proteins: current structural insights. Mol Pharmacol 2007;72(2):219-30.


20. Johnston CA, Temple BR, Chen JG, Gao Y, Moriyama EN, Jones AM, Siderovski DP, Willard FS. Comment on "A G protein coupled receptor is a plasma membrane receptor for the plant hormone abscisic acid". Science 2007;318(5852):914; author reply 914.

19. Uhlik M, Temple B, Bencharit S, Kimple A, Siderovski DP, Johnson GL. Structural and evolutionary division of phosphotyrosine binding (PTB) domains. J Mol Biol 2005;345(1):1-20.

18. McCudden CR, Hains MD, Kimple RJ, Siderovski DP, Willard FS. G-protein signaling: back to the future. Cell Mol Life Sci 2005;62(5):551-77.

17. Siderovski DP, Willard FS. The GAPs, GEFs, and GDIs of heterotrimeric G-protein alpha subunits. Int J Biol Sci 2005;1(2):51-66.

16. Willard FS, Kimple RJ, Siderovski DP. Return of the GDI: the GoLoco motif in cell division. Annu Rev Biochem 2004;73:925-51.

15. Jones MB, Siderovski DP, Hooks SB. The G betagamma dimer as a novel source of selectivity in G-protein signaling: GGL-ing at convention. Mol Interv 2004;4(4):200-14.

14. Willard FS, Kimple RJ, Kimple AJ, Johnston CA, Siderovski DP. Fluorescence-based assays for RGS box function. Methods Enzymol 2004;389:56-71.

13. Hains MD, Siderovski DP, Harden TK. Application of RGS box proteins to evaluate G-protein selectivity in receptor-promoted signaling. Methods Enzymol 2004;389:71-88.

12. Willard FS, Siderovski DP. Purification and in vitro functional analysis of the Arabidopsis thaliana regulator of G-protein signaling-1. Methods Enzymol 2004;389:320-38.

11. Martin-McCaffrey L, Willard FS, Pajak A, Dagnino L, Siderovski DP, D'Souza SJ. Analysis of interactions between regulator of G-protein signaling-14 and microtubules. Methods Enzymol 2004;390:240-58.

10. Kimple RJ, Willard FS, Siderovski DP. Purification and in vitro functional analyses of RGS12 and RGS14 GoLoco motif peptides. Methods Enzymol 2004;390:416-36.

9. Kimple RJ, Jones MB, Shutes A, Yerxa BR, Siderovski DP, Willard FS. Established and emerging fluorescence-based assays for G-protein function: heterotrimeric G-protein alpha subunits and regulator of G-protein signaling (RGS) proteins. Comb Chem High Throughput Screen 2003;6(4):399-407.

8. Rojas RJ, Kimple RJ, Rossman KL, Siderovski DP, Sondek J. Established and emerging fluorescence-based assays for G-protein function: Ras-superfamily GTPases. Comb Chem High Throughput Screen 2003;6(4):409-18.

7. Siderovski DP, Snow BE, Chung S, Brothers GM, Sondek J, Betts L. Assays of complex formation between RGS protein G gamma subunit-like domains and G beta subunits. Methods Enzymol 2002;344:702-23.

6. Snow BE, Brothers GM, Siderovski DP. Molecular cloning of regulators of G-protein signaling family members and characterization of binding specificity of RGS12 PDZ domain. Methods Enzymol 2002;344:740-61.

5. Neubig RR, Siderovski DP. Regulators of G-protein signalling as new central nervous system drug targets. Nat Rev Drug Discov 2002;1(3):187-97.

4. Kimple RJ, Willard FS, Siderovski DP. The GoLoco motif: heralding a new tango between G protein signaling and cell division. Mol Interv 2002;2(2):88-100.


3. Sondek J, Siderovski DP. Ggamma-like (GGL) domains: new frontiers in G-proteinsignaling and beta-propeller scaffolding. Biochem Pharmacol 2001;61(11):1329-37.

2. Siderovski DP, Diverse-Pierluissi M, De Vries L. The GoLoco motif: a Galphai/o bindingmotif and potential guanine-nucleotide exchange factor. TiBS 1999;24(9):340-1.

1. Siderovski DP, Strockbine B, Behe CI. Whither goest the RGS proteins? Crit RevBiochem Mol Biol 1999;34(4):215-51.

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