Bradley A Katz

Summary

Affiliation: Celera Genomics
Country: USA

Publications

  1. ncbi request reprint Expression, crystallization, and three-dimensional structure of the catalytic domain of human plasma kallikrein
    Jie Tang
    Department of Structural Chemistry, Celera Genomics, South San Francisco, California 94080, USA
    J Biol Chem 280:41077-89. 2005
  2. ncbi request reprint Factor VIIa inhibitors: gaining selectivity within the trypsin family
    William D Shrader
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:1596-600. 2006
  3. ncbi request reprint Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors
    Bradley A Katz
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    J Mol Biol 329:93-120. 2003
  4. ncbi request reprint Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA)
    Bradley A Katz
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    J Mol Biol 344:527-47. 2004
  5. ncbi request reprint Contribution of multicentered short hydrogen bond arrays to potency of active site-directed serine protease inhibitors
    Bradley A Katz
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    J Am Chem Soc 124:11657-68. 2002
  6. ncbi request reprint Factor VIIa inhibitors: improved pharmacokinetic parameters
    Aleksandr Kolesnikov
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2243-6. 2006
  7. ncbi request reprint 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
    Jeffrey R Spencer
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 12:2023-6. 2002
  8. ncbi request reprint 2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
    Richard L Mackman
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 12:2019-22. 2002
  9. ncbi request reprint Discovery of novel heterocyclic factor VIIa inhibitors
    Roopa Rai
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2270-3. 2006
  10. ncbi request reprint Small molecule inhibitors of plasma kallikrein
    Wendy B Young
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2034-6. 2006

Collaborators

Detail Information

Publications14

  1. ncbi request reprint Expression, crystallization, and three-dimensional structure of the catalytic domain of human plasma kallikrein
    Jie Tang
    Department of Structural Chemistry, Celera Genomics, South San Francisco, California 94080, USA
    J Biol Chem 280:41077-89. 2005
    ....
  2. ncbi request reprint Factor VIIa inhibitors: gaining selectivity within the trypsin family
    William D Shrader
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:1596-600. 2006
    ....
  3. ncbi request reprint Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors
    Bradley A Katz
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    J Mol Biol 329:93-120. 2003
    ....
  4. ncbi request reprint Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA)
    Bradley A Katz
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    J Mol Biol 344:527-47. 2004
    ..The 6-fluoro-5-amidinobenzimidzole, CA-11, is more than 1000-fold selective against natural Ala190 protease anti-targets, and more than 100-fold selective against other Ser190 anti-targets...
  5. ncbi request reprint Contribution of multicentered short hydrogen bond arrays to potency of active site-directed serine protease inhibitors
    Bradley A Katz
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    J Am Chem Soc 124:11657-68. 2002
    ..These features suggest little covalent nature within the short hydrogen bonds, despite their extraordinary shortness (as short as 2.0 A)...
  6. ncbi request reprint Factor VIIa inhibitors: improved pharmacokinetic parameters
    Aleksandr Kolesnikov
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2243-6. 2006
    ..Small structural modifications to existing leads allow the modulation of half-life and clearance, potentially making these compounds suitable candidates for drug development...
  7. ncbi request reprint 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
    Jeffrey R Spencer
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 12:2023-6. 2002
    ..The structure-based design of potent and selective urokinase-type plasminogen activator (uPA) inhibitors with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described...
  8. ncbi request reprint 2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
    Richard L Mackman
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 12:2019-22. 2002
    ..The development of potent and selective urokinase-type plasminogen activator (uPA) inhibitors based on the lead molecule 2-(2-hydroxy-3-ethoxyphenyl)-1H-benzimidazole-5-carboxamidine (3a) is described...
  9. ncbi request reprint Discovery of novel heterocyclic factor VIIa inhibitors
    Roopa Rai
    Celera, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2270-3. 2006
    ..In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold...
  10. ncbi request reprint Small molecule inhibitors of plasma kallikrein
    Wendy B Young
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2034-6. 2006
    ..Herein, we describe the SAR and structural binding modes of a series of inhibitors of plasma kallikrein as well as the pharmacokinetics of a lead analog 11 in rat...
  11. ncbi request reprint Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases
    John R Somoza
    Celera, 180 Kimball Way, South San Francisco, CA 94080 USA
    Structure 12:1325-34. 2004
    ..This work sheds light on the catalytic mechanism of the HDACs, and on differences in substrate specificity across the HDAC family. The structure also suggests how phosphorylation of Ser39 affects HDAC8 activity...
  12. ncbi request reprint Structure-guided design of peptide-based tryptase inhibitors
    Mary E McGrath
    Celera Genomics, Inc, 180 Kimball Way, South San Francisco, California 94080, USA
    Biochemistry 45:5964-73. 2006
    ..Thus, replacement of Lys/Arg at P1 in a peptide-like scaffold does not need to be accompanied by a loss in target affinity...
  13. ncbi request reprint The structure of the extracellular region of human hepsin reveals a serine protease domain and a novel scavenger receptor cysteine-rich (SRCR) domain
    John R Somoza
    Celera, Inc, 180 Kimball Road, South San Francisco, CA 94080, USA
    Structure 11:1123-31. 2003
    ..The structure suggests how the extracellular region of hepsin may be positioned with respect to the plasma membrane...
  14. ncbi request reprint Factor VIIa inhibitors: chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model
    Wendy B Young
    Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2037-41. 2006
    ..Results for heparin and enoxaparin (Lovenox) in the baboon model are also presented...