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Features of selective kinase inhibitors.

by: ZA Knight, KM Shokat
Chem Biol, Vol. 12, No. 6. (June 2005), pp. 621-637.


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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.


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