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The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.
Wu, Jiang-Ping; Wang, Ji; Abeywardane, Asitha; Andersen, Denise; Emmanuel, Michel; Gautschi, Elda; Goldberg, Daniel R; Kashem, Mohammed A; Lukas, Susan; Mao, Wang; Martin, Leslie; Morwick, Tina; Moss, Neil; Pargellis, Christopher; Patel, Usha R; Patnaude, Lori; Peet, Gregory W; Skow, Donna; Snow, Roger J; Ward, Yancey; Werneburg, Brian; White, Andre.
Affiliation
  • Wu JP; Research and Development, Boehringer-Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA. jwu@rdg.boehringer-ingelheim.com
Bioorg Med Chem Lett ; 17(16): 4664-9, 2007 Aug 15.
Article in En | MEDLINE | ID: mdl-17576063
ABSTRACT
The discovery of a series of potent, carboline-based MK2 inhibitors is described. 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.
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Collection: 01-internacional Database: MEDLINE Main subject: Carbolines / Protein Serine-Threonine Kinases / Intracellular Signaling Peptides and Proteins Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2007 Document type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Carbolines / Protein Serine-Threonine Kinases / Intracellular Signaling Peptides and Proteins Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2007 Document type: Article Affiliation country: United States