Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor
SC Koeberle, J Romir, S Fischer, A Koeberle… - Nature chemical …, 2012 - nature.com
SC Koeberle, J Romir, S Fischer, A Koeberle, V Schattel, W Albrecht, C Grütter, O Werz…
Nature chemical biology, 2012•nature.comUntil 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 vi vo 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.
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 vi vo 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.
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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