Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

  • Nat Chem Biol. 2011 Dec 25;8(2):141-3. doi: 10.1038/nchembio.761.
Solveigh C Koeberle  1 ,  Johannes Romir ,  Stefan Fischer ,  Andreas Koeberle ,  Verena Schattel ,  Wolfgang Albrecht ,  Christian Grütter ,  Oliver Werz ,  Daniel Rauh ,  Thilo Stehle ,  Stefan A Laufer
Affiliations
  • 1. Institute of Pharmacy, University of Tübingen, Tübingen, Germany.
PMID: 22198732 DOI: 10.1038/nchembio.761
Abstract

Until now, a lack of inhibitors with high potency and selectivity in vivo has hampered investigation of the p38 mitogen-activated protein kinase (MAPK) signaling pathway. We describe the design of skepinone-L, which is, to our knowledge, the first ATP-competitive p38 MAPK Inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chemical biology research, and it may foster the development of a unique class of kinase inhibitors.

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