B Govinda Rao

Summary

Affiliation: Vertex Pharmaceuticals
Country: USA

Publications

  1. ncbi Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies
    B Govinda Rao
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA E mail
    Curr Pharm Des 11:295-322. 2005
  2. ncbi Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides
    B Govinda Rao
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 17:2250-3. 2007
  3. ncbi In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061
    Chao Lin
    Vertex Pharmaceuticals Incorporated, Cambridge, Massachusetts 02139, USA
    J Biol Chem 280:36784-91. 2005
  4. pmc Phenotypic characterization of resistant Val36 variants of hepatitis C virus NS3-4A serine protease
    Yi Zhou
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA
    Antimicrob Agents Chemother 52:110-20. 2008
  5. ncbi Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization
    Robert B Perni
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 14:1441-6. 2004
  6. ncbi Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones
    Upul K Bandarage
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:44-8. 2008
  7. pmc Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease
    Robert B Perni
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, Massachusetts 02139, USA
    Antimicrob Agents Chemother 50:899-909. 2006
  8. ncbi Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants
    Robert B Perni
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 14:1939-42. 2004
  9. ncbi Phenotypic and structural analyses of hepatitis C virus NS3 protease Arg155 variants: sensitivity to telaprevir (VX-950) and interferon alpha
    Yi Zhou
    Vertex Pharmaceuticals Inc, Cambridge, Massachusetts 02139, USA
    J Biol Chem 282:22619-28. 2007
  10. pmc In vitro phenotypic characterization of hepatitis C virus NS3 protease variants observed in clinical studies of telaprevir
    Min Jiang
    Vertex Pharmaceuticals Incorporated, Cambridge, Massachusetts, USA
    Antimicrob Agents Chemother 57:6236-45. 2013

Collaborators

Detail Information

Publications14

  1. ncbi Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies
    B Govinda Rao
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA E mail
    Curr Pharm Des 11:295-322. 2005
    ..Pros and cons of inhibitors with non-hydroxamate Zinc-binding groups in terms of specificity, toxicity and pharmacokinetic properties are discussed...
  2. ncbi Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides
    B Govinda Rao
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 17:2250-3. 2007
    ..In particular, compound 4b has shown excellent in vitro potency against the isolated TACE enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 4b bound to TACE was obtained...
  3. ncbi In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061
    Chao Lin
    Vertex Pharmaceuticals Incorporated, Cambridge, Massachusetts 02139, USA
    J Biol Chem 280:36784-91. 2005
    ..Both cross-resistance mutations (A156V and A156T) displayed significantly diminished fitness (or replication capacity) in a transient replicon cell system...
  4. pmc Phenotypic characterization of resistant Val36 variants of hepatitis C virus NS3-4A serine protease
    Yi Zhou
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA
    Antimicrob Agents Chemother 52:110-20. 2008
    ..Finally, the sensitivity of these replicon variants to alpha interferon or ribavirin remained unchanged compared to that of the wild-type...
  5. ncbi Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization
    Robert B Perni
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 14:1441-6. 2004
    ..The alpha-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3.4A protease inhibitors. Structure-activity relationships and prime side optimization are discussed...
  6. ncbi Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones
    Upul K Bandarage
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:44-8. 2008
    ..In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 8b in complex with TACE was also obtained...
  7. pmc Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease
    Robert B Perni
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, Massachusetts 02139, USA
    Antimicrob Agents Chemother 50:899-909. 2006
    ..Therefore, the overall preclinical profile of VX-950 supports its candidacy as a novel oral therapy against hepatitis C...
  8. ncbi Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants
    Robert B Perni
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 14:1939-42. 2004
    ..4A enzyme...
  9. ncbi Phenotypic and structural analyses of hepatitis C virus NS3 protease Arg155 variants: sensitivity to telaprevir (VX-950) and interferon alpha
    Yi Zhou
    Vertex Pharmaceuticals Inc, Cambridge, Massachusetts 02139, USA
    J Biol Chem 282:22619-28. 2007
    ..Finally, these variant replicons were shown to have reduced replication capacity compared with the wild-type HCV replicon in cells...
  10. pmc In vitro phenotypic characterization of hepatitis C virus NS3 protease variants observed in clinical studies of telaprevir
    Min Jiang
    Vertex Pharmaceuticals Incorporated, Cambridge, Massachusetts, USA
    Antimicrob Agents Chemother 57:6236-45. 2013
    ..In general, the replication capacity of telaprevir-resistant variants was lower than that of the wild-type replicon. ..
  11. ncbi In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms
    Chao Lin
    Vertex Pharmaceuticals Inc, Cambridge, Massachusetts 02139, USA
    J Biol Chem 279:17508-14. 2004
    ..Modeling analysis suggests that there are different mechanisms of resistance to VX-950 and BILN 2061...
  12. ncbi Viral and cellular RNA helicases as antiviral targets
    Ann D Kwong
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, Massachusetts 02139, USA
    Nat Rev Drug Discov 4:845-53. 2005
    ....
  13. ncbi Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants
    Robert B Perni
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 13:4059-63. 2003
    ..4A protease without the need of a charged functionality. An aldehyde is used as a prototype reversible electrophilic warhead. The SAR of the P1 and P2 inhibitor positions is discussed...
  14. doi FURSMASA: a new approach to rapid scoring functions that uses a MD-averaged potential energy grid and a solvent-accessible surface area term with parameters GA fit to experimental data
    David A Pearlman
    Vertex Pharmaceuticals, 130 Waverly Street, Cambridge, Massachusetts 02139 4242, USA
    Proteins 71:1519-38. 2008
    ..10,000 decoys), p38 (502 actives vs. 10,000 decoys), and HIV (787 actives vs. 10,000 decoys) used in earlier work to critically evaluate many popular scoring functions, and find that FURSMASA performs surprisingly well for IMPDH and HIV...