Article
Discovery of selective irreversible inhibitors for EGFR-T790M.
Bioorganic & medicinal chemistry letters - 15 Jan 2011
Zhou Wenjun, Ercan Dalia, Jänne Pasi A, Gray Nathanael S
Abstract excerpt
Targeting the epidermal growth factor receptor kinase (EGFR) with ATP-competitive kinase inhibitors results in dramatic but short-lived responses in patients with EGFR mutant non small cell lung cancer. A series of novel covalent EGFR kinase inhibitors with selectivity for the clinically relevant T790M 'gatekeeper' resistance mutation relative to wild-type EGFR were discovered by library screening. A...
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