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Small‐Molecule Kinase‐Inhibitor Target Assessment
Author(s) -
Kung Charles,
Shokat Kevan M.
Publication year - 2005
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200400393
Subject(s) - drug discovery , protein kinase inhibitor , kinase , small molecule , computational biology , identification (biology) , chemical genetics , drug target , protein kinase a , biology , chemistry , biochemistry , botany
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.