Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor |
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Authors: | Koeberle Solveigh C Romir Johannes Fischer Stefan Koeberle Andreas Schattel Verena Albrecht Wolfgang Grütter Christian Werz Oliver Rauh Daniel Stehle Thilo Laufer Stefan A |
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Affiliation: | Institute of Pharmacy, University of Tübingen, Tübingen, Germany. |
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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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