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  • Title: Small-molecule kinase-inhibitor target assessment.
    Author: Kung C, Shokat KM.
    Journal: Chembiochem; 2005 Mar; 6(3):523-6. PubMed ID: 15696508.
    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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