Guohua Zhao

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. doi request reprint Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists
    Guohua Zhao
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 23:3914-9. 2013
  2. doi request reprint Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors
    Guohua Zhao
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 23:1622-5. 2013
  3. ncbi request reprint Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
    Guohua Zhao
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:309-12. 2004
  4. ncbi request reprint Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
    Guohua Zhao
    Department of Discovery Chemistry, Bristol Myers Squibb, Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 15:3992-5. 2005
  5. ncbi request reprint Synthesis of potent and highly selective inhibitors of human tryptase
    William A Slusarchyk
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3235-8. 2002
  6. ncbi request reprint Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase
    Gregory S Bisacchi
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:2227-31. 2004
  7. doi request reprint Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold
    Scott A Bolton
    Bristol Myers Squibb Research and Development, Hopewell, NJ 08534 5400, USA
    Bioorg Med Chem Lett 23:5239-43. 2013
  8. ncbi request reprint Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
    Ligaya M Simpkins
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 17:6476-80. 2007
  9. ncbi request reprint Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
    James C Sutton
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3229-33. 2002
  10. pmc Biosynthesis of covalently bound flavin: isolation and in vitro flavinylation of the monomeric sarcosine oxidase apoprotein
    Alshaimaa Hassan-Abdallah
    Department of Biochemistry and Molecular Biology, College of Medicine, Drexel University, Philadelphia, Pennsylvania 19102, USA
    Biochemistry 44:6452-62. 2005

Collaborators

Detail Information

Publications16

  1. doi request reprint Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists
    Guohua Zhao
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 23:3914-9. 2013
    ..Several members of this series were identified as potent 5-HT2C receptor agonists with high functional selectivity against the 5-HT2A and 5-HT2B receptors and reduced food intake in an acute rat feeding model upon oral dosing...
  2. doi request reprint Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors
    Guohua Zhao
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 23:1622-5. 2013
    ....
  3. ncbi request reprint Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
    Guohua Zhao
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:309-12. 2004
    ..A member of this series, 8t, was identified as a potent inhibitor of human tryptase (IC(50)=38 nM) with selectivity >/=330-fold versus related serine proteases (trypsin, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa) [corrected]...
  4. ncbi request reprint Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
    Guohua Zhao
    Department of Discovery Chemistry, Bristol Myers Squibb, Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 15:3992-5. 2005
    ..Synthesis and structure-activity relationships of a series of substituted diprolyl nitriles are described, leading to the identification of compound 1 with a measured DPP4 K(i) of 3.6 nM...
  5. ncbi request reprint Synthesis of potent and highly selective inhibitors of human tryptase
    William A Slusarchyk
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3235-8. 2002
    ..7 nM) with high selectivity (>3000-fold) for tryptase versus related serine proteases including trypsin...
  6. ncbi request reprint Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase
    Gregory S Bisacchi
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 14:2227-31. 2004
    ..In particular, BMS-354326 (4) is a highly potent tryptase inhibitor (IC(50)=1.8 nM), which has excellent selectivity against trypsin and most other related serine proteases...
  7. doi request reprint Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold
    Scott A Bolton
    Bristol Myers Squibb Research and Development, Hopewell, NJ 08534 5400, USA
    Bioorg Med Chem Lett 23:5239-43. 2013
    ..In an unanticipated result, the m-benzamide P1 (compounds 21a and 21b) proved to be a viable benzamidine replacement, albeit with a 20-40 fold loss in potency against factor VIIa. ..
  8. ncbi request reprint Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
    Ligaya M Simpkins
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 17:6476-80. 2007
    ..A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold...
  9. ncbi request reprint Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
    James C Sutton
    The Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 12:3229-33. 2002
    ....
  10. pmc Biosynthesis of covalently bound flavin: isolation and in vitro flavinylation of the monomeric sarcosine oxidase apoprotein
    Alshaimaa Hassan-Abdallah
    Department of Biochemistry and Molecular Biology, College of Medicine, Drexel University, Philadelphia, Pennsylvania 19102, USA
    Biochemistry 44:6452-62. 2005
    ..The reconstituted enzyme contains a modified cysteine-flavin linkage (8-nor-8-S-cysteinyl) as compared with native MSOX (8alpha-S-cysteinyl), a difference that may account for its approximately 10-fold lower catalytic activity...
  11. doi request reprint Covalent flavinylation of monomeric sarcosine oxidase: identification of a residue essential for holoenzyme biosynthesis
    Alshaimaa Hassan-Abdallah
    Department of Biochemistry and Molecular Biology, Drexel University, College of Medicine, Philadelphia, Pennsylvania 19102, USA
    Biochemistry 47:1136-43. 2008
    ..The results show that a basic residue at position 49 is essential for covalent flavinylation of MSOX and suggest that Arg49 also plays an important role in sarcosine oxidation...
  12. doi request reprint Arginine 49 is a bifunctional residue important in catalysis and biosynthesis of monomeric sarcosine oxidase: a context-sensitive model for the electrostatic impact of arginine to lysine mutations
    Alshaimaa Hassan-Abdallah
    Department of Biochemistry and Molecular Biology, Drexel University College of Medicine, Philadelphia, Pennsylvania 19102, USA
    Biochemistry 47:2913-22. 2008
    ..A context-sensitive model for the electrostatic impact of an arginine to lysine mutation can account for the dramatically different consequences of the Arg49Lys mutation on MSOX catalysis and holoenzyme biosysnthesis...
  13. pmc Identification of the oxygen activation site in monomeric sarcosine oxidase: role of Lys265 in catalysis
    Guohua Zhao
    Department of Biochemistry and Molecular Biology, Drexel University College of Medicine, Philadelphia, Pennsylvania 19102, USA
    Biochemistry 47:9124-35. 2008
    ..Significantly, the active sites for sarcosine oxidation and oxygen reduction are located on opposite faces of the flavin ring...
  14. ncbi request reprint NF90 regulates cell cycle exit and terminal myogenic differentiation by direct binding to the 3'-untranslated region of MyoD and p21WAF1/CIP1 mRNAs
    Lingfang Shi
    Division of Pulmonary and Critical Care Medicine, Stanford University Medical Center, Stanford, California 94305 5236, USA
    J Biol Chem 280:18981-9. 2005
    ..NF90 regulates transcription factors and a cell cycle inhibitor essential for skeletal muscle differentiation and for survival...
  15. ncbi request reprint Simvastatin rescues rats from fatal pulmonary hypertension by inducing apoptosis of neointimal smooth muscle cells
    Toshihiko Nishimura
    Division of Pulmonary and Critical Care Medicine, Stanford University Medical Center, Stanford, Calif 94305 5236, USA
    Circulation 108:1640-5. 2003
    ..The present study was undertaken to investigate the efficacy of simvastatin and its mechanism of reversing established neointimal vascular occlusion and pulmonary hypertension...
  16. pmc Dynamic binding of Ku80, Ku70 and NF90 to the IL-2 promoter in vivo in activated T-cells
    Lingfang Shi
    Pulmonary and Critical Care Medicine, Stanford University Medical Center, Stanford, CA 94305 5236, USA
    Nucleic Acids Res 35:2302-10. 2007
    ..Dynamic changes in binding of Ku80, Ku70 and NF90 to the IL-2 proximal promoter in vivo correlate with chromatin remodeling and transcriptional initiation in activated T-cells...