Features of selective kinase inhibitors

被引:522
作者
Knight, ZA [1 ]
Shokat, KM [1 ]
机构
[1] Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
来源
CHEMISTRY & BIOLOGY | 2005年 / 12卷 / 06期
关键词
D O I
10.1016/j.chembiol.2005.04.011
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
Small-molecule inhibitors of protein and lipid kinases have emerged as indispensable tools for studying signal transduction. Despite the widespread use of these reagents, there is little consensus about the biochemical criteria that define their potency and selectivity in cells. We discuss some of the features that determine the cellular activity of kinase inhibitors and propose a framework for interpreting inhibitor selectivity.
引用
收藏
页码:621 / 637
页数:17
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