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Author Details

Robert J Fletterick
University of California San Francisco
1971
269
81
Andrej Sali (CM4AI)
PMIDPaper TitleJournal TitlePublished Year
30853418Covalent Modification and Regulation of the Nuclear Receptor Nurr1 by a Dopamine Metabolite.Cell Chem Biol2019
30305617LRH-1 mitigates intestinal inflammatory disease by maintaining epithelial homeostasis and cell survival.Nat Commun2018
28981251Development of 5N-Bicalutamide, a High-Affinity Reversible Covalent Antiandrogen.ACS Chem Biol2017
28445593NR5A2 discovering compounds that block tumor growth in PDAC.J Surg Oncol2017
26829219Dlx5 Homeodomain:DNA Complex: Structure, Binding and Effect of Mutations Related to Split Hand and Foot Malformation Syndrome.J Mol Biol2016
27467220Disulfide-Trapping Identifies a New, Effective Chemical Probe for Activating the Nuclear Receptor Human LRH-1 (NR5A2).PLoS One2016
25499868Advances in our structural understanding of orphan nuclear receptors.Trends Biochem Sci2015
26653140A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver.Elife2015
26416531Structure of Liver Receptor Homolog-1 (NR5A2) with PIP3 hormone bound in the ligand binding pocket.J Struct Biol2015
26207810The FKBP52 Cochaperone Acts in Synergy with β-Catenin to Potentiate Androgen Receptor Signaling.PLoS One2015
25825768Structure-based discovery of NANOG variant with enhanced properties to promote self-renewal and reprogramming of pluripotent stem cells.Proc Natl Acad Sci U S A2015
25675535Silencing LRH-1 in colon cancer cell lines impairs proliferation and alters gene expression programs.Proc Natl Acad Sci U S A2015
25686748Histone demethylase KDM5A is regulated by its reader domain through a positive-feedback mechanism.Nat Commun2015
24906004Computer modeling of a newly identified THRB gene mutation (S350L) associated with resistance to thyroid hormone in three unrelated patients.Thyroid2014
25288771The signaling phospholipid PIP3 creates a new interaction surface on the nuclear receptor SF-1.Proc Natl Acad Sci U S A2014
24927529Structural and functional insight into TAF1-TAF7, a subcomplex of transcription factor II D.Proc Natl Acad Sci U S A2014
24936658The human orphan nuclear receptor tailless (TLX, NR2E1) is druggable.PLoS One2014
23806029Incidental identification of a thyroid hormone receptor beta (THRB) gene variant in a family with autoimmune thyroid disease.Thyroid2013
23667258Structure-based discovery of antagonists of nuclear receptor LRH-1.J Biol Chem2013
23805258Plant Kinesin-Like Calmodulin Binding Protein Employs Its Regulatory Domain for Dimerization.PLoS One2013
21878368A conserved surface on the ligand binding domain of nuclear receptors for allosteric control.Mol Cell Endocrinol2012
22984442Structure of a novel winged-helix like domain from human NFRKB protein.PLoS One2012
22187462Structural basis of coactivation of liver receptor homolog-1 by β-catenin.Proc Natl Acad Sci U S A2012
21730179Targeting the regulation of androgen receptor signaling by the heat shock protein 90 cochaperone FKBP52 in prostate cancer cells.Proc Natl Acad Sci U S A2011
21949357Nuclear receptor liver receptor homologue 1 (LRH-1) regulates pancreatic cancer cell growth and proliferation.Proc Natl Acad Sci U S A2011
20335180Hormone binding and co-regulator binding to the glucocorticoid receptor are allosterically coupled.J Biol Chem2010
21041940Decoration of microtubules in solution by the kinesin-14, Ncd.Acta Crystallogr D Biol Crystallogr2010
20493816Conformation switching of clathrin light chain regulates clathrin lattice assembly.Dev Cell2010
20179344Accommodation of structural rearrangements in the huntingtin-interacting protein 1 coiled-coil domain.Acta Crystallogr D Biol Crystallogr2010
18988706Structure of SF-1 bound by different phospholipids: evidence for regulatory ligands.Mol Endocrinol2009
19416847Structure of the complex of a mitotic kinesin with its calcium binding regulator.Proc Natl Acad Sci U S A2009
18798561Molecular basis for dimer formation of TRbeta variant D355R.Proteins2009
18513992Structural dynamics of the microtubule binding and regulatory elements in the kinesin-like calmodulin binding protein.J Struct Biol2008
18790740Actin binding by Hip1 (huntingtin-interacting protein 1) and Hip1R (Hip1-related protein) is regulated by clathrin light chain.J Biol Chem2008
187546106-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor.J Med Chem2008
19015525The structure of corepressor Dax-1 bound to its target nuclear receptor LRH-1.Proc Natl Acad Sci U S A2008
17502099The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family.Structure2007
23484530Perspectives on designs of antiandrogens for prostate cancer.Expert Opin Drug Discov2007
17918822Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.J Med Chem2007
18007036Interaction between the androgen receptor and a segment of its corepressor SHP.Acta Crystallogr D Biol Crystallogr2007
17823305Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor.Mol Endocrinol2007
17278355Ca ion and the troponin switch.Adv Exp Med Biol2007
16469331An atomic model of the thin filament in the relaxed and Ca2+-activated states.J Mol Biol2006
16804159A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding.Sci STKE2006
16962610Directed evolution of an anti-prion protein scFv fragment to an affinity of 1 pM and its structural interpretation.J Mol Biol2006
16864794Structural basis for unique mechanisms of folding and hemoglobin binding by a malarial protease.Proc Natl Acad Sci U S A2006
16415057Dynamics of the C-terminal region of TnI in the troponin complex in solution.Biophys J2006
15707893Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1.Cell2005
16263725Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators.J Biol Chem2005
16359432Molecular modelling of the androgen receptor axis: rational basis for androgen receptor intervention in androgen-independent prostate cancer.BJU Int2005
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Collaborators

Department of Pharmaceutical Chemistry, University of California san francisco
Co-authored papers 37
University of California san francisco
Co-authored papers 13
Weill Institute for Neurosciences, University of California San Francisco
Co-authored papers 11
Hoag Memorial Hospital Presbyterian
Co-authored papers 9
Duke Molecular Physiology Institute
Co-authored papers 7
The Joint Center for Structural Genomics, Stanford University
Co-authored papers 6
Sandler Center for Drug Discovery, University of California San Francisco
Co-authored papers 6
Accelero Biostructures Inc., USA XPose Therapeutics Inc.
Co-authored papers 5
University of California san francisco
Co-authored papers 5
Joint Center for Structural Genomics
Co-authored papers 4
Department of Pharmaceutical Chemistry, University of California san francisco
Co-authored papers 4
The Scripps Research Institute, USA The Skaggs Institute for Chemical Biology
Co-authored papers 3
Accelero Biostructures Inc., USA XPose Therapeutics Inc.
Co-authored papers 3
Joint Center for Structural Genomics
Co-authored papers 3
Co-authored papers 2
University of California Riverside
Co-authored papers 2
Institute of Biochemistry & Cell Biology
Co-authored papers 2
University of California at San Francisco
Co-authored papers 2
University of East Anglia
Co-authored papers 2
Co-authored papers 2
Merck & Co., Inc.
Co-authored papers 2
St. Jude Children's Research Hospital
Co-authored papers 2
Co-authored papers 2
Columbia University Irving Medical Center
Co-authored papers 2
University of Washington
Co-authored papers 2
National Centre for Cell Science, SP Pune University Campus
Co-authored papers 2
Gladstone Institutes
Co-authored papers 2
University of California, USA Quantitative Biosciences Institute (QBI) san francisco
Co-authored papers 2
Joint Center for Structural Genomics
Co-authored papers 2
University of California Riverside School of Medicine
Co-authored papers 1