Article
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.
Nature chemical biology - 1 Apr 2007
Blair Jimmy A, Rauh Daniel, Kung Charles, Yun Cai-Hong, Fan Qi-Wen, Rode Haridas, Zhang Chao, Eck Michael J, Weiss William A, Shokat Kevan M
Abstract excerpt
As key components in nearly every signal transduction pathway, protein kinases are attractive targets for the regulation of cellular signaling by small-molecule inhibitors. We report the structure-guided development of 6-acrylamido-4-anilinoquinazoline irreversible kinase inhibitors that potently and selectively target rationally designed kinases bearing two selectivity elements that are not found together in any...
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