Illuminating the Druggable Genome - Funded Research

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Pilot Projects Investigating Understudied G Protein-Coupled Receptors, Ion Channels, and Protein Kinases (R03 Clinical Trial Not Allowed) RFA-RM-22-024
PI Name	Institution Name	Title
ALDINGER, KIMBERLY ANNE	SEATTLE CHILDREN'S HOSPITAL	Defining the MAST4 interactome in brain development and epilepsy
BHATNAGAR, SUSHANT (contact) KIMPLE, MICHELLE E	UNIVERSITY OF ALABAMA AT BIRMINGHAM	Investigating the Effects of ADGRB3 Signaling on Incretin-Mediated Insulin Secretion from Pancreatic Beta-Cells
BRASCH, JULIA	UNIVERSITY OF UTAH	Structural and functional characterization of synaptic adhesion GPCR ADGRB3 binding interactions
CALDWELL, KIM A	UNIVERSITY OF ALABAMA IN TUSCALOOSA	Functional analysis of KCNK12 in dopaminergic neuroprotection
CHEN, RONG	WAKE FOREST UNIVERSITY HEALTH SCIENCES	Illumination of TAAR2 Location, Function and Regulators
CHOI, SUYONG	UNIVERSITY OF NEBRASKA MEDICAL CENTER	PIP5K1A is a novel mutant KRAS effector and essential for pancreatic cancer cell survival
COETZEE, WILLIAM A (contact) FESKE, STEFAN	NEW YORK UNIVERSITY SCHOOL OF MEDICINE	Tweety proteins: their roles in pericytes and macrophages
CUELLO, LUIS GONZALO	TEXAS TECH UNIVERSITY HEALTH SCIS CENTER	Utilizing the power of synthetic biology and De Novo design for the overexpression and biochemical stabilization of KCNA6 or Kv1.6 potassium channels in the E. coli expression system
CUI, TAIXING	UNIVERSITY OF SOUTH CAROLINA AT COLUMBIA	Cyclin-dependent kinase (CDK)19-mediated vein graft intimal hyperplasia
GARCIA, VICTOR	NEW YORK MEDICAL COLLEGE	Uncovering the role of GPR75 as an activator of fatty acid transporters in non-alcoholic fatty liver disease (NAFLD)
GELMANN, EDWARD P	UNIVERSITY OF ARIZONA	DYRK1B Inhibition for Prostate Cancer
KANT, SHASHI	BRIGHAM AND WOMEN'S HOSPITAL	Mixed Lineage Kinase 2 (MLK2) and vascular homeostasis
KEMP, CHRISTOPHER J	FRED HUTCHINSON CANCER CENTER	Mechanisms of Pip4k2c and Pip5k1b dependencies in Ras driven squamous cell carcinoma
RESSL, SUSANNE	UNIVERSITY OF TEXAS AT AUSTIN	The biophysical basis of the ADGRB3 extra-cellular interaction network.
SATO, PRISCILA	DREXEL UNIVERSITY	Deciphering a novel kinase function for adck2 in the heart
SCHURER, STEPHAN C	UNIVERSITY OF MIAMI SCHOOL OF MEDICINE	Elucidating the Understudied Kinase PNCK as a Prospective Drug Target in Renal Cell Carcinoma
TANIS, JESSICA E	UNIVERSITY OF DELAWARE	Impact of PIP5K1 on extracellular vesicle biogenesis
TERENTYEV, DMITRY A	OHIO STATE UNIVERSITY	Defining the role of KCNN1 in atrial arrhythmias
VETTER, STEFAN W	NORTH DAKOTA STATE UNIVERSITY	Biochemical Characterization of the CAMKV Pseudokinase
WEIS, WILLIAM I	STANFORD UNIVERSITY	Nanobody- and mini-G protein-enabled molecular pharmacology of HCAR1
WONG, CHING-ON	RUTGERS THE STATE UNIV OF NJ NEWARK	The role of TTYH1 in glial cell autophagy

Pilot Projects Investigating Understudied G Protein-Coupled Receptors, Ion Channels, and Protein Kinases (R03 Clinical Trial Not Allowed) RFA-RM-21-012
PI Name	Institution Name	Title
CAO, ERHU	UNIVERSITY OF UTAH	Develop enabling biochemical and structural tools for dissecting the roles of PKD2L2 in metabolism
DELLING, MARKUS G	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Functional characterization of the dark matter ion channel polycystin2-like2
FESKE, STEFAN (contact) COETZEE, WILLIAM A	NEW YORK UNIVERSITY SCHOOL OF MEDICINE	FAM26F function and role in macrophages
JACKSON, PETER KENT	STANFORD UNIVERSITY	Understudied GPCRs connecting signaling in primary cilia to obesity and metabolic disease
KHAN, MOHD NAZIR	EMORY UNIVERSITY	Targeting GPR68 as a novel modulator of osteoarthritis
KU, GREGORY MICHAEL	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Creating a mouse and human model of a novel monogenic diabetes syndrome
MA, ZHENGYU	ALFRED I. DU PONT HOSP FOR CHILDREN	Identify cell surface protein ligand candidates for understudied adhesion GPCRs using a sensitive cell-based approach
NAKAGAWA, TERUNAGA	VANDERBILT UNIVERSITY	Illuminating the structure and function of CACNG5 and 7
ORLANDI, CESARE	UNIVERSITY OF ROCHESTER	Orphan Receptor Gprc5b in Retinoic Acid-induced Affective Behaviors
PROBER, DAVID AARON (contact) CHOU, TSUI-FEN	CALIFORNIA INSTITUTE OF TECHNOLOGY	Phosphoproteomic Analyses of Understudied Protein Kinases that affect Zebrafish Sleep
SACK, JON THOMAS (contact) FERNS, MICHAEL J	UNIVERSITY OF CALIFORNIA AT DAVIS	Generation of tools for visualizing understudied KvS potassium channel proteins
SHEPARD, BLYTHE D	GEORGETOWN UNIVERSITY	Hepatic GPR125: ligands and liver repair
SINGH, HARPREET	OHIO STATE UNIVERSITY	Biophysical properties and role of CLIC6 in cardiomyocyte mitochondria
THYME, SUMMER B	UNIVERSITY OF ALABAMA AT BIRMINGHAM	Role of VRK2 Kinase in Brain Development and Function
TOWLER, DWIGHT A	UT SOUTHWESTERN MEDICAL CENTER	Cdc42bpg signaling in arteriosclerosis and vascular fibrosis
TURK, BENJAMIN E	YALE UNIVERSITY	Defining protein interaction networks involving the atypical MAP kinases ERK4 and ERK7
WANG, BIAO	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	TSSK-dependent signaling pathway in spermatogenesis
YOUNG, SAMUEL MATTHEW	UNIVERSITY OF IOWA	Elucidating the roles of CACNA2D2 and CACNA2D3 in presynaptic regulation of mammalian synaptic function
YU, EUGENE	ROSWELL PARK CANCER INSTITUTE CORP	CRISPR-mediated engineering and pilot study of mouse mutants of the bitter taste receptor genes
ZAGOTTA, WILLIAM N	UNIVERSITY OF WASHINGTON	Functional and structural dynamics of KCNH4 and KCNH8

Cutting Edge Informatics Tools for Illuminating the Druggable Genome (U01 Clinical Trial Not Allowed) RFA-RM-21-020
PI Name	Institution Name	Title
KANNAN, NATARAJAN (contact) LU, WEI.	UNIVERSITY OF GEORGIA	Annotating dark ion-channel functions using evolutionary features, machine learning and knowledge graph mining
PANDEY, GAURAV (contact) SCHLESSINGER, AVNER	ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI	Multi-modal data integration to identify kinase substrates
ZHANG, BING	BAYLOR COLLEGE OF MEDICINE	Illuminating understudied druggable proteins using pan-cancer proteogenomics data

Pilot Projects Investigating Understudied G Protein-Coupled Receptors, Ion Channels, and Protein Kinases (R03 Clinical Trial Not Allowed) RFA-RM-20-019
PI Name	Institution Name	Title
BANERJEE, PRIYA R	STATE UNIVERSITY OF NEW YORK AT BUFFALO	Deciphering the role of low complexity domains in dual specificity kinase function
BOBECK, ERIN NICOLE	UTAH STATE UNIVERSITY	GPR171 As a Novel Target to Treat Neuropathic Pain
BRETT, THOMAS JOHN	WASHINGTON UNIVERSITY	Illuminating the role of chloride channel regulator CLCA4 in TMEM16 Family potentiation and disease
CARON, KATHLEEN M	UNIV OF NORTH CAROLINA CHAPEL HILL	Illuminating Orphan GPCRs in Lymphatics
CHANG, GEOFFREY A (contact) INSEL, PAUL A	UNIVERSITY OF CALIFORNIA, SAN DIEGO	Nanobody inhibitors of proton-sensing G protein-coupled receptors
COLECRAFT, HENRY M	COLUMBIA UNIVERSITY HEALTH SCIENCES	Nanobodies for Probing CACNA2D2 and CACNA2D3 Function, Expression, and Therapeutics
GAUTRON, LAURENT	UT SOUTHWESTERN MEDICAL CENTER	Neuronal GPR149 and energy homeostasis
GERBER, SCOTT A	DARTMOUTH COLLEGE	Proteomics approaches for illuminating the functions of the dark kinases Nek6, Nek7 & Nek9
GRUETER, CHAD E	UNIVERSITY OF IOWA	Cdk19-dependent transcriptional mechanisms in cardiac hypertrophy
HAMMOND, GERALD R	UNIVERSITY OF PITTSBURGH AT PITTSBURGH	PIP5K1A as a novel driver of PI3K signaling in health and disease
KHOR, BERNARD	BENAROYA RESEARCH INST AT VIRGINIA MASON	Illuminating a novel role of understudied DYRKs in anti-inflammatory T cell differentiation
LEE, SUN JOO	WASHINGTON UNIVERSITY	Structure/function analysis of understudied pH-sensitive Kir4.2 channels in vitro with conformation specific nanobodies
MACLEAN, DAVID MALCOM	UNIVERSITY OF ROCHESTER	Genetic code expansion and the study of CACNG proteins
MAIERS, JESSICA L	MAYO CLINIC ROCHESTER	Identifying targetable mechanisms of TMEM38B/TRIC-B in liver fibrosis
MYERS, BENJAMIN	UNIVERSITY OF UTAH	Illuminating Druggable Targets via Interrogation of Direct GPCR-kinase Interactions
NAIRN, ANGUS C	YALE UNIVERSITY	Role of MAST3 kinase in developmental and epileptic encephalopathy
PABLA, NAVJOT	OHIO STATE UNIVERSITY	Illuminating the biological functions of CDKL1 Kinase
REITER, JEREMY F	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Illuminating the function of the understudied kinase DYRK2 in ciliary Hedgehog signal transduction
SANTY, LORRAINE C	PENNSYLVANIA STATE UNIVERSITY-UNIV PARK	Identifying endosomal Phosphatidylinositol 4-phosphate 5-kinase isoforms regulating growth factor stimulated integrin recycling and migration
SUTTON, LAURIE	UNIVERSITY OF MARYLAND BALT CO CAMPUS	Investigating the role of GPR162 in hedonic behaviors
TRAYNELIS, STEPHEN F	EMORY UNIVERSITY	Genetic analysis to determine the functional role of GRID1
VARSHNEY, GAURAV K	OKLAHOMA MEDICAL RESEARCH FOUNDATION	Functional characterization of understudied protein kinases implicated in developmental disorders using zebrafish
WANDINGER-NESS, ANGELA (contact) HUDSON, LAURIE G	UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR	Illuminating the functions and translational potential of CDC42BP/MRCK kinases in ovarian cancer
ZHANG, CHENG	UNIVERSITY OF PITTSBURGH AT PITTSBURGH	Structure and pharmacology of GPR32 in the resolution of inflammation

Pilot Projects Investigating Understudied G Protein-Coupled Receptors, Ion Channels, and Protein Kinases (R03 Clinical Trial Not Allowed) RFA-RM-19-011
PI Name	Institution Name	Title
BUROW, MATTHEW E. (contact) DREWRY, DAVID HAROLD	TULANE UNIVERSITY OF LOUISIANA	Characterization of an understudied kinase, NEK5, in acquisition of a mesenchymal and migratory cell
FOSKETT, JAMES KEVIN	UNIVERSITY OF PENNSYLVANIA	Identification of CALHM proteins as ion channels
GLIMCHER, LAURIE HOLLIS	DANA-FARBER CANCER INST	Multi-faceted Roles of an Atypical Kinase RIOK2 in Erythropoiesis and Myelodyplastic Syndromes
GOETZ, SARAH	DUKE UNIVERSITY	Defining biochemical mechanisms of dominant interference by disease-causing variants of TTBK2
GOLKOWSKI, MARTIN	UNIVERSITY OF WASHINGTON	Targeting understudied kinases in cancer cell plasticity and drug resistance
HAHN, WILLIAM C	DANA-FARBER CANCER INST	Novel genetic dependencies in VRK2 methylated glioblastoma multiforme
JIN, CHUNYANG (contact) HESK, DAVID	RESEARCH TRIANGLE INSTITUTE	Preparation and characterization of radioligands for the orphan receptor GPR88
JO, YOUNG-HWAN	ALBERT EINSTEIN COLLEGE OF MEDICINE	Role of HCAR1 in glucose homeostasis
JURA, NATALIA	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Structural and functional investigation of the understudied HIPK1 kinase
MANGLIK, AASHISH	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Biochemical approaches to enlighten GPR85 function
MARTINELLI, DAVID CHRISTOPHER	UNIVERSITY OF CONNECTICUT SCH OF MED/DNT	Determination of the subcellular localization of adhesion G protein-coupled receptor B3 (ADGRB3) and its locations of interaction with secreted C1Q-like ligands
NGUYEN, THUY	RESEARCH TRIANGLE INSTITUTE	Development of Novel Neuropeptide B/W Receptor 1 Agonists
PHILIPS, MARK REID	NEW YORK UNIVERSITY SCHOOL OF MEDICINE	Regulation of KRAS Trafficking and Signaling by GPR31
REN, HONGXIA (contact) WATTS, VAL J	INDIANA UNIV-PURDUE UNIV AT INDIANAPOLIS	Illuminating the Metabolic Function of GPR162 by Delineating Downstream Signaling Pathways and Characterizing Hypothalamic Expression Pattern
SODEN, MARTA E	UNIVERSITY OF WASHINGTON	Targeted mutagenesis to elucidate the function of understudied ion channels in the central nervous system
TERSEY, SARAH A. (contact) MIRMIRA, RAGHAVENDRA G	UNIVERSITY OF CHICAGO	The 12-HETE receptor Gpr31 in the β-cell pathogenesis of type 1 diabetes
TSAI, NIEN-PEI	UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN	Study of PAK3 in epilepsy-associated defects in synaptic plasticity

Pilot Projects Investigating Understudied G Protein-Coupled Receptors, Ion Channels, and Protein Kinases (R03 Clinical Trial Not Allowed) RFA-RM-18-021
PI Name	Institution Name	Title
ARAC-OZKAN, DEMET	UNIVERSITY OF CHICAGO	Structural and Functional Studies of Brain Angiogenesis Inhibitors (BAIs/ADGRBs)
CHAHROUR, MARIA	UT SOUTHWESTERN MEDICAL CENTER	Investigating the role of BCKDK in neurodevelopmental disorders through a novel mouse model
DEVI, LAKSHMI A	ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI	Targeted Deorphanization of G Protein-Coupled Receptors
FESKE, STEFAN	NEW YORK UNIVERSITY SCHOOL OF MEDICINE	Calcium channel CACNB1 in T cell function and immunity
GREEN, THOMAS ARTHUR (contact) LAEZZA, FERNANDA	UNIVERSITY OF TEXAS MED BR GALVESTON	Gpr12: a novel factor for addiction and mental health
ISOM, DANIEL	UNIVERSITY OF MIAMI SCHOOL OF MEDICINE	New CRISPR-based technologies for screening dark GPCRs
KU, GREGORY MICHAEL	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Uncovering Two Novel Diabetes Drug Targets in the IDG
LEE, AMY	UNIVERSITY OF IOWA	Illuminating the functions of CACNA2D4 in the brain
LODMELL, J STEPHEN	UNIVERSITY OF MONTANA	Role of the atypical protein kinase RIOK3 in the cellular antiviral response
MARTO, JARROD A	DANA-FARBER CANCER INST	Tools for the understudied kinase PNK3
NEWTON, ALEXANDRA C	UNIVERSITY OF CALIFORNIA, SAN DIEGO	Establishing Function of Understudied PRKCQ Kinase in Cellular Regulation and Disease
SEBAG, JULIEN ALBERT	UNIVERSITY OF IOWA	Identification of the central localization and regulation of the Prokineticin 1 Receptor, a novel target for the treatment of obesity
TAYLOR, SUSAN S	UNIVERSITY OF CALIFORNIA, SAN DIEGO	Illuminating the Role of understudied PRKACB Splice Variants in PKA Signaling
TURK, BENJAMIN E (contact) CALDERWOOD, DAVID A	YALE UNIVERSITY	Interaction of substrates and inhibitors with tousled-like kinase 2
WHIM, MATTHEW	LSU HEALTH SCIENCES CENTER	Determining the role of the adrenal Y2 and Y5 receptors in the prevention of hypoglycemia
WHITEHURST, ANGELIQUE WRIGHT	UT SOUTHWESTERN MEDICAL CENTER	Mechanisms and Models of Testis Specific Serine Kinase 6 (TSSK6)

Cutting Edge Informatics Tools for Illuminating the Druggable Genome (U01 Clinical Trial Not Allowed) RFA-RM-18-011
PI Name	Institution Name	Title
KANNAN, NATARAJAN (contact) KOCHUT, KRZYSZTOF J.	UNIVERSITY OF GEORGIA	A data analytics framework for mining the dark kinome
ROBINSON, PETER NICHOLAS (contact) MUNGALL, CHRISTOPHER J OPREA, TUDOR I	JACKSON LABORATORY	Illuminating the Druggable Genome by Knowledge Graphs
WU, GUANMING (contact) DEUSTACHIO, PETER G STEIN, LINCOLN D.	OREGON HEALTH & SCIENCE UNIVERSITY	Reactome IDG portal: Pathway-based analysis and visualization of understudied human proteins

Knowledge Management Center for Illuminating the Druggable Genome (U24) RFA-RM-16-024
PI Name	Institution Name	Title
MA'AYAN, AVI	ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI	Knowledge Management Center for Illuminating the Druggable Genome (Component Award)
OPREA, TUDOR I	UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR	Knowledge Management Center for Illuminating the Druggable Genome (Center Award)

Data and Resource Generation Centers for Illuminating the Druggable Genome (U24) RFA-RM-16-026
PI Name	Institution Name	Title
JOHNSON, GARY L	UNIV OF NORTH CAROLINA CHAPEL HILL	Illuminating Function of the Understudied Druggable Kinome
MCMANUS, MICHAEL T (contact) JAN, LILY Y	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Illuminating Druggable Dark Matter
ROTH, BRYAN L. (contact) SHOICHET, BRIAN K	UNIV OF NORTH CAROLINA CHAPEL HILL	Illuminating the druggable GPCR-ome

Resource Dissemination and Outreach Center for Illuminating the Druggable Genome (U24) RFA-RM-16-025
PI Name	Institution Name	Title
SCHÜRER, STEPHAN C (contact) OPREA, TUDOR I SKLAR, LARRY A.	UNIVERSITY OF MIAMI SCHOOL OF MEDICINE	Illuminating the Druggable Genome Resource Dissemination and Outreach Center (IDG-RDOC)

Development of a Knowledge Management Center for Illuminating the Druggable GenomeTitle Here (U54) RFA-RM-13-011
PI Name	Institution Name	Title
MA'AYAN, AVI	ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI	Mount Sinais Knowledge Management Center for Illuminating the Druggable Genome
OPREA, TUDOR I	UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR	Illuminating the Druggable Genome Knowledge Management Center (IDG KMC)

Adaptation of Scalable Technologies to Illuminate the Druggable Genome (U01) RFA-RM-13-010
PI Name	Institution Name	Title
FINKBEINER, STEVEN M.	J. DAVID GLADSTONE INSTITUTES	Physical Exam of Human Neurons to Identify Functions of the Druggable Genome
JOHNSON, GARY L.	UNIV OF NORTH CAROLINA CHAPEL HILL	Activation and Regulation of the Understudied Kinome Using MIB/MS Technology
MCMANUS, MICHAEL T.	UNIVERSITY OF CALIFORNIA, SAN FRANCISCO	Unlocking the Hidden Kinome
QIN, JUN	BAYLOR COLLEGE OF MEDICINE	Signaling Networks of Nuclear Receptor Transcriptional Crosstalk in Lung Cancer
ROTH, BRYAN L (contact) SHOICHET, BRIAN K.	UNIV OF NORTH CAROLINA CHAPEL HILL	Scalable technologies for illuminating the druggable GPCR-ome
TOMITA, SUSUMU	YALE UNIVERSITY	Identify functional modulators of ionotropic neurotransmitter receptors in brain
YEH, JING-RUEY JOANNA (contact) KOKEL, DAVID	MASSACHUSETTS GENERAL HOSPITAL	Scalable in vivo tools for annotating and manipulating the druggable genome