Albert C Pierce

Summary

Affiliation: Vertex Pharmaceuticals
Country: USA

Publications

  1. ncbi Kinase inhibitors and the case for CH...O hydrogen bonds in protein-ligand binding
    Albert C Pierce
    Vertex Pharmaceuticals, Cambridge, Massachusetts 02139, USA
    Proteins 49:567-76. 2002
  2. ncbi BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease
    Albert C Pierce
    Vertex Pharmaceuticals, 130 Waverly Street, Cambridge, Massachusetts 02139
    J Med Chem 47:2768-75. 2004
  3. ncbi CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor
    Albert C Pierce
    Vertex Pharmaceuticals, Inc, 130 Waverly Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 48:1278-81. 2005
  4. ncbi Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase
    Albert C Pierce
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA
    J Med Chem 51:1972-5. 2008
  5. ncbi Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia
    Robert J Davies
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, Massachusetts 02139, United States
    J Med Chem 54:7184-92. 2011
  6. ncbi Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase
    Ron Grey
    Vertex Pharmaceuticals Incorporated, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 19:3019-22. 2009
  7. ncbi Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole
    Tiansheng Wang
    Vertex Pharmaceuticals Inc, Cambridge, Massachusetts 02139 4242, USA
    J Med Chem 52:7938-41. 2009
  8. ncbi 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
    Mark W Ledeboer
    Vertex Pharmaceuticals Inc, Cambridge, MA 02139 4242, United States
    Bioorg Med Chem Lett 19:6529-33. 2009
  9. ncbi A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors
    Tiansheng Wang
    Vertex Pharmaceuticals Inc, 130 Waverly St, Cambridge, MA 02139 4242, United States
    Bioorg Med Chem Lett 20:153-6. 2010

Collaborators

Detail Information

Publications9

  1. ncbi Kinase inhibitors and the case for CH...O hydrogen bonds in protein-ligand binding
    Albert C Pierce
    Vertex Pharmaceuticals, Cambridge, Massachusetts 02139, USA
    Proteins 49:567-76. 2002
    ..Such knowledge will be of considerable value in protein modeling, ligand design, and structure-activity analysis...
  2. ncbi BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease
    Albert C Pierce
    Vertex Pharmaceuticals, 130 Waverly Street, Cambridge, Massachusetts 02139
    J Med Chem 47:2768-75. 2004
    ..In an era of increasingly high-throughput structural biology, such methods for high-throughput utilization of structural information will become increasingly valuable...
  3. ncbi CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor
    Albert C Pierce
    Vertex Pharmaceuticals, Inc, 130 Waverly Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 48:1278-81. 2005
    ..Understanding the importance of these CH...O and CH...N hydrogen bonds allowed the design of a novel quinazolin-4-ylthiazol-2-ylamine inhibitor of GSK3 with a structurally confirmed CH...O hydrogen bond to the protein...
  4. ncbi Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase
    Albert C Pierce
    Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA
    J Med Chem 51:1972-5. 2008
    ..091 and 4.5 microM. This gives a 14-fold enrichment over the earlier HTS run, and the two crystal structures solved confirmed the binding modes predicted by docking...
  5. ncbi Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia
    Robert J Davies
    Vertex Pharmaceuticals Inc, 130 Waverly Street, Cambridge, Massachusetts 02139, United States
    J Med Chem 54:7184-92. 2011
    ....
  6. ncbi Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase
    Ron Grey
    Vertex Pharmaceuticals Incorporated, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 19:3019-22. 2009
    ..This resulted in compound 29, a selective, soluble and permeable inhibitor of Pim-1...
  7. ncbi Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole
    Tiansheng Wang
    Vertex Pharmaceuticals Inc, Cambridge, Massachusetts 02139 4242, USA
    J Med Chem 52:7938-41. 2009
    ..The compound is further evaluated for its ability to block the EPO/JAK2 signaling cascade in vitro and in vivo...
  8. ncbi 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
    Mark W Ledeboer
    Vertex Pharmaceuticals Inc, Cambridge, MA 02139 4242, United States
    Bioorg Med Chem Lett 19:6529-33. 2009
    ..Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2...
  9. ncbi A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors
    Tiansheng Wang
    Vertex Pharmaceuticals Inc, 130 Waverly St, Cambridge, MA 02139 4242, United States
    Bioorg Med Chem Lett 20:153-6. 2010
    ..SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors...