Robert J Fletterick

Summary

Affiliation: University of California
Country: USA

Publications

  1. doi request reprint Perspectives on designs of antiandrogens for prostate cancer
    Eva Estebanez-Perpina
    University of California San Francisco, Department of Biochemistry and Biophysics, San Francisco, CA941432240, USA 1 415 476 5051 1 415 476 1902
    Expert Opin Drug Discov 2:1341-55. 2007
  2. pmc Molecular basis for dimer formation of TRbeta variant D355R
    Natalia Jouravel
    Department of Biochemistry and Biophysics, University of California San Francisco UCSF, San Francisco, California 94158, USA
    Proteins 75:111-7. 2009
  3. pmc Structural basis of coactivation of liver receptor homolog-1 by β-catenin
    Fumiaki Yumoto
    Department of Biochemistry and Biophysics, University of California San Francisco, 600 16th Street, San Francisco, CA 94158, USA
    Proc Natl Acad Sci U S A 109:143-8. 2012
  4. pmc The structure of corepressor Dax-1 bound to its target nuclear receptor LRH-1
    Elena P Sablin
    Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 105:18390-5. 2008
  5. ncbi request reprint Interaction between the androgen receptor and a segment of its corepressor SHP
    Natalia Jouravel
    Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA
    Acta Crystallogr D Biol Crystallogr 63:1198-200. 2007
  6. pmc Structure-based discovery of antagonists of nuclear receptor LRH-1
    Cindy Benod
    Department of Biochemistry and Biophysics, University of California at San Francisco, San Francisco, California 94158, USA
    J Biol Chem 288:19830-44. 2013
  7. pmc Structure of SF-1 bound by different phospholipids: evidence for regulatory ligands
    Elena P Sablin
    Department of Biochemistry and Biophysics, University of California, San Francisco, California 94143, USA
    Mol Endocrinol 23:25-34. 2009
  8. pmc A surface on the androgen receptor that allosterically regulates coactivator binding
    Eva Estebanez-Perpina
    Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 104:16074-9. 2007
  9. pmc 6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor
    Leslie A Cruz
    Graduate Program in Chemistry and Chemical Biology, University of California San Francisco, San Francisco, California 94158 2517, USA
    J Med Chem 51:5856-60. 2008
  10. pmc Conformation switching of clathrin light chain regulates clathrin lattice assembly
    Jeremy D Wilbur
    Graduate Program in Biophysics, University of California, San Francisco, San Francisco, CA 94143, USA
    Dev Cell 18:841-8. 2010

Collaborators

Detail Information

Publications12

  1. doi request reprint Perspectives on designs of antiandrogens for prostate cancer
    Eva Estebanez-Perpina
    University of California San Francisco, Department of Biochemistry and Biophysics, San Francisco, CA941432240, USA 1 415 476 5051 1 415 476 1902
    Expert Opin Drug Discov 2:1341-55. 2007
    ..The challenges to designing these compounds are significant but so is the potential for treatment of the disease...
  2. pmc Molecular basis for dimer formation of TRbeta variant D355R
    Natalia Jouravel
    Department of Biochemistry and Biophysics, University of California San Francisco UCSF, San Francisco, California 94158, USA
    Proteins 75:111-7. 2009
    ....
  3. pmc Structural basis of coactivation of liver receptor homolog-1 by β-catenin
    Fumiaki Yumoto
    Department of Biochemistry and Biophysics, University of California San Francisco, 600 16th Street, San Francisco, CA 94158, USA
    Proc Natl Acad Sci U S A 109:143-8. 2012
    ..The LRH-1 binding site in β-catenin is also required for association with androgen receptor, providing evidence that the observed LRH-1/β-catenin interaction may be prototypic...
  4. pmc The structure of corepressor Dax-1 bound to its target nuclear receptor LRH-1
    Elena P Sablin
    Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 105:18390-5. 2008
    ..The structure of the Dax-1:LRH-1 complex provides the molecular mechanism for the function of Dax-1 as a potent transcriptional repressor...
  5. ncbi request reprint Interaction between the androgen receptor and a segment of its corepressor SHP
    Natalia Jouravel
    Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA
    Acta Crystallogr D Biol Crystallogr 63:1198-200. 2007
    ..Comparisons of AR structures bound to coactivator peptides and the SHP peptide revealed structural similarity of their binding sites, suggesting that transcriptional AR activity may be inhibited by SHP by competing with AR coactivators...
  6. pmc Structure-based discovery of antagonists of nuclear receptor LRH-1
    Cindy Benod
    Department of Biochemistry and Biophysics, University of California at San Francisco, San Francisco, California 94158, USA
    J Biol Chem 288:19830-44. 2013
    ..Our data suggest that specific antagonists of LRH-1 could be used as specific molecular probes for elucidating the roles of the receptor in different types of malignancies. ..
  7. pmc Structure of SF-1 bound by different phospholipids: evidence for regulatory ligands
    Elena P Sablin
    Department of Biochemistry and Biophysics, University of California, San Francisco, California 94143, USA
    Mol Endocrinol 23:25-34. 2009
    ....
  8. pmc A surface on the androgen receptor that allosterically regulates coactivator binding
    Eva Estebanez-Perpina
    Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 104:16074-9. 2007
    ..Mutation of residues that form BF-3 inhibits AR function and AR AF-2 activity. We propose that BF-3 is a previously unrecognized allosteric regulatory site needed for AR activity in vivo and a possible pharmaceutical target...
  9. pmc 6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor
    Leslie A Cruz
    Graduate Program in Chemistry and Chemical Biology, University of California San Francisco, San Francisco, California 94158 2517, USA
    J Med Chem 51:5856-60. 2008
    ..Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705...
  10. pmc Conformation switching of clathrin light chain regulates clathrin lattice assembly
    Jeremy D Wilbur
    Graduate Program in Biophysics, University of California, San Francisco, San Francisco, CA 94143, USA
    Dev Cell 18:841-8. 2010
    ....
  11. pmc Nuclear receptor liver receptor homologue 1 (LRH-1) regulates pancreatic cancer cell growth and proliferation
    Cindy Benod
    Department of Biochemistry and Biophysics, University of California 600 16th Street, GH S412E, San Francisco, CA 94158 2517, USA
    Proc Natl Acad Sci U S A 108:16927-31. 2011
    ..This study demonstrates the critical involvement of LRH-1 in development and progression of pancreatic cancer, suggesting the LRH-1 receptor as a plausible therapeutic target for treatment of pancreatic ductal adenocarcinomas...
  12. ncbi request reprint Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor
    Eva Estebanez-Perpina
    Department of Biochemistry and Biophysics, University of California, San Francisco, California 94158 2240, USA
    Mol Endocrinol 21:2919-28. 2007
    ..DHPPA represents a novel class of potent TRbeta antagonist, and its crystal structure suggests new ways to design antagonists that target the assembly of nuclear hormone receptor gene-regulatory complexes and block transcription...