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

被引：104

作者：

Koeberle, Solveigh C. ^{[2
,3
]}

Romir, Johannes ^{[1
]}

Fischer, Stefan ^{[2
]}

Koeberle, Andreas ^{[4
]}

Schattel, Verena ^{[2
]}

Albrecht, Wolfgang ^{[5
]}

Gruetter, Christian ^{[6
]}

Werz, Oliver ^{[4
]}

Rauh, Daniel ^{[6
]}

Stehle, Thilo ^{[1
,7
]}

Laufer, Stefan A. ^{[2
]}

机构：

[1] Univ Tubingen, Interfac Inst Biochem, Tubingen, Germany

[2] Univ Tubingen, Inst Pharm, Tubingen, Germany

[3] Fritz Lipmann Inst, Inst Age Res, Jena, Germany

[4] Univ Jena, Inst Pharm, Jena, Germany

[5] CAIR Biosci GmbH, Tubingen, Germany

[6] Tech Univ Dortmund, Fac Chem Chem Biol, Dortmund, Germany

[7] Vanderbilt Univ, Sch Med, Dept Pediat, Nashville, TN 37212 USA

来源：

NATURE CHEMICAL BIOLOGY | 2012年 / 8卷 / 02期

关键词：

MAP KINASE; SIGNALING PATHWAYS; KAPPA-B; CELLS; EXPRESSION; ADHESION; DESIGN; INFLAMMATION; PLAYS;

D O I：

10.1038/nchembio.761

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：141 / 143

页数：3

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