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Chembiochem. 2005 Mar;6(3):523-6.

Small-molecule kinase-inhibitor target assessment.

Author information

1
Chemistry and Chemical Biology Graduate Program, University of California, San Francisco, CA 94143, USA.

Abstract

The identification of the cellular targets of small-molecule protein kinase inhibitors is a significant hurdle to assessing their therapeutic potential for many diseases. Here we review several biochemical and genetics-based approaches to identifying inhibitor targets. We also describe a chemical-genomics approach to kinase-inhibitor target identification and validation that matches transcriptional signatures elicited by a drug of unknown specificity and those elicited by highly specific pharmacological inhibition of engineered candidate kinase targets.

PMID:
15696508
DOI:
10.1002/cbic.200400393
[Indexed for MEDLINE]

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