title: Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.
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.
authors.affiliation: Institute of Pharmacy, University of Tübingen, Tübingen, Germany.
authors.forename: Solveigh C
authors.initials: SC
authors.lastname: Koeberle
authors.forename: Johannes
authors.initials: J
authors.lastname: Romir
authors.forename: Stefan
authors.initials: S
authors.lastname: Fischer
authors.forename: Andreas
authors.initials: A
authors.lastname: Koeberle
authors.forename: Verena
authors.initials: V
authors.lastname: Schattel
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Albrecht
authors.forename: Christian
authors.initials: C
authors.lastname: Grütter
authors.forename: Oliver
authors.initials: O
authors.lastname: Werz
authors.forename: Daniel
authors.initials: D
authors.lastname: Rauh
authors.forename: Thilo
authors.initials: T
authors.lastname: Stehle
authors.forename: Stefan A
authors.initials: SA
authors.lastname: Laufer
mesh_terms: D000255:Adenosine Triphosphate; D000818:Animals; D001667:Binding, Competitive; D003986:Dibenzocycloheptenes / Q000737:chemistry*; D015195:Drug Design; D051379:Mice; D008958:Models, Molecular; D054730:Protein Interaction Domains and Motifs; D047428:Protein Kinase Inhibitors / Q000737:chemistry*; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
chemical_list: D003986:Dibenzocycloheptenes; D047428:Protein Kinase Inhibitors; C572387:skepinone-L; D000255:Adenosine Triphosphate; D048051:p38 Mitogen-Activated Protein Kinases