Robert X Xu

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi request reprint A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer
    Robert X Xu
    Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Mol Cell 16:919-28. 2004
  2. ncbi request reprint Crystal structures of the catalytic domain of phosphodiesterase 4B complexed with AMP, 8-Br-AMP, and rolipram
    Robert X Xu
    Department of Computational, Analytical and Structural Sciences, GlaxoSmithKline, 5 Moore Drive, V 180, Research Triangle Park, NC 27709, USA
    J Mol Biol 337:355-65. 2004
  3. doi request reprint Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist
    Barry G Shearer
    Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 53:1857-61. 2010
  4. ncbi request reprint Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 16:1788-94. 2006
  5. doi request reprint Discovery of a novel class of PPARdelta partial agonists
    Barry G Shearer
    Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 18:5018-22. 2008
  6. ncbi request reprint Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1
    Irina N Krylova
    Department of Physiology, University of California, San Francisco, California 94143, USA
    Cell 120:343-55. 2005
  7. ncbi request reprint Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents
    Michael L Sierra
    Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25 27 Avenue du Québec, 91951 Les Ulis, France, USA
    J Med Chem 50:685-95. 2007
  8. ncbi request reprint Crystallization of cyclic nucleotide phosphodiesterases
    Hengming Ke
    Department of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, USA
    Methods Mol Biol 307:181-90. 2005

Collaborators

Detail Information

Publications8

  1. ncbi request reprint A structural basis for constitutive activity in the human CAR/RXRalpha heterodimer
    Robert X Xu
    Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Mol Cell 16:919-28. 2004
    ..Insights into the molecular basis of CAR constitutive activity can be exploited in the design of inverse agonists as drugs for treatment of obesity...
  2. ncbi request reprint Crystal structures of the catalytic domain of phosphodiesterase 4B complexed with AMP, 8-Br-AMP, and rolipram
    Robert X Xu
    Department of Computational, Analytical and Structural Sciences, GlaxoSmithKline, 5 Moore Drive, V 180, Research Triangle Park, NC 27709, USA
    J Mol Biol 337:355-65. 2004
    ..8-Br-AMP binds in the syn conformation to the enzyme and demonstrates an alternative nucleotide-binding mode. Rolipram occupies much of the AMP-binding site and forms two hydrogen bonds with Gln443 similar to the nucleotides...
  3. doi request reprint Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist
    Barry G Shearer
    Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 53:1857-61. 2010
    ..Compound 3 is a PPARdelta antagonist with utility as a tool to elucidate PPARdelta cell biology and pharmacology...
  4. ncbi request reprint Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385
    John F Miller
    GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 16:1788-94. 2006
    ..Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385...
  5. doi request reprint Discovery of a novel class of PPARdelta partial agonists
    Barry G Shearer
    Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 18:5018-22. 2008
    ..The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells...
  6. ncbi request reprint Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1
    Irina N Krylova
    Department of Physiology, University of California, San Francisco, California 94143, USA
    Cell 120:343-55. 2005
    ..We propose that phospholipids regulate gene expression by directly binding to NR5A nuclear receptors...
  7. ncbi request reprint Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents
    Michael L Sierra
    Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25 27 Avenue du Québec, 91951 Les Ulis, France, USA
    J Med Chem 50:685-95. 2007
    ..Compound 25a (GW590735) has been progressed to clinical trials for the treatment of diseases of lipid imbalance...
  8. ncbi request reprint Crystallization of cyclic nucleotide phosphodiesterases
    Hengming Ke
    Department of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, USA
    Methods Mol Biol 307:181-90. 2005
    ..Finally, we discuss detailed procedures for and pitfalls of the crystallization of PDEs, which may be valuable for crystallization of other PDE members...