doi: 10.1002/cbic.200400393.
Small-molecule kinase-inhibitor target assessment
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- PMID: 15696508
- DOI: 10.1002/cbic.200400393
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Small-molecule kinase-inhibitor target assessment
Chembiochem.
2005 Mar.
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.
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