Christopher Pargellis

Summary

Affiliation: Boehringer Ingelheim

Publications

  1. ncbi Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
    Christopher Pargellis
    Department of Biology, Boehringer Ingelheim Pharmaceuticals, Research and Development Center, 900 Ridgebury Road, Ridgefield, Connecticut 06877, USA
    Nat Struct Biol 9:268-72. 2002
  2. ncbi The non-diaryl heterocycle classes of p38 MAP kinase inhibitors
    Pier F Cirillo
    Departments of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA
    Curr Top Med Chem 2:1021-35. 2002
  3. ncbi Discovery and characterization of a substrate selective p38alpha inhibitor
    Walter Davidson
    Department of Immunology and Inflammation, Boehringer Ingelheim Pharmaceuticals, Research and Development Center, 900 Ridgebury Road, Ridgefield, Connecticut 06877, USA
    Biochemistry 43:11658-71. 2004
  4. ncbi The discovery of carboline analogs as potent MAPKAP-K2 inhibitors
    Jiang Ping Wu
    Research and Development, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA
    Bioorg Med Chem Lett 17:4664-9. 2007
  5. ncbi Discovery and optimization of p38 inhibitors via computer-assisted drug design
    Daniel R Goldberg
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, Research and Development Center, Ridgefield, Connecticut 06877, USA
    J Med Chem 50:4016-26. 2007
  6. ncbi Inhibitors of p38 mitogen-activated protein kinase for the treatment of rheumatoid arthritis
    Christopher Pargellis
    Department of Immunology Inflammation Chemistry, Boehringer Ingelheim Pharmaceuticals Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA
    Curr Opin Investig Drugs 4:566-71. 2003

Detail Information

Publications6

  1. ncbi Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
    Christopher Pargellis
    Department of Biology, Boehringer Ingelheim Pharmaceuticals, Research and Development Center, 900 Ridgebury Road, Ridgefield, Connecticut 06877, USA
    Nat Struct Biol 9:268-72. 2002
    ..One of the most potent compounds in this series, BIRB 796, has picomolar affinity for the kinase and low nanomolar inhibitory activity in cell culture...
  2. ncbi The non-diaryl heterocycle classes of p38 MAP kinase inhibitors
    Pier F Cirillo
    Departments of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA
    Curr Top Med Chem 2:1021-35. 2002
    ..At least one of these classes requires the kinase to undergo reorganization prior to binding. From this diverse set of inhibitors four compounds have been reported advancing into human clinical trials...
  3. ncbi Discovery and characterization of a substrate selective p38alpha inhibitor
    Walter Davidson
    Department of Immunology and Inflammation, Boehringer Ingelheim Pharmaceuticals, Research and Development Center, 900 Ridgebury Road, Ridgefield, Connecticut 06877, USA
    Biochemistry 43:11658-71. 2004
    ....
  4. ncbi The discovery of carboline analogs as potent MAPKAP-K2 inhibitors
    Jiang Ping Wu
    Research and Development, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA
    Bioorg Med Chem Lett 17:4664-9. 2007
    ..These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a...
  5. ncbi Discovery and optimization of p38 inhibitors via computer-assisted drug design
    Daniel R Goldberg
    Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc, Research and Development Center, Ridgefield, Connecticut 06877, USA
    J Med Chem 50:4016-26. 2007
    ..Integration of computational methods, X-ray crystallography, and structure-activity relationships will be disclosed, which lead to a new class of p38 inhibitors that bind to p38 MAP kinase in a Phe out conformation...
  6. ncbi Inhibitors of p38 mitogen-activated protein kinase for the treatment of rheumatoid arthritis
    Christopher Pargellis
    Department of Immunology Inflammation Chemistry, Boehringer Ingelheim Pharmaceuticals Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA
    Curr Opin Investig Drugs 4:566-71. 2003
    ..Several other p38 inhibitors are currently undergoing phase I clinical trials...