Features of selective kinase inhibitors.
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.
Knight
Zachary A
ZA
Program in Chemistry and Chemical Biology, University of California-San Francisco, San Francisco, CA 94143, USA.
Shokat
Kevan M
KM
D000818:Animals; D004353:Drug Evaluation, Preclinical; D006801:Humans; D010744:Phosphoric Monoester Hydrolases / Q000378:metabolism*; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013379:Substrate Specificity
D047428:Protein Kinase Inhibitors; D010744:Phosphoric Monoester Hydrolases