Article
Noncovalent wild-type-sparing inhibitors of EGFR T790M.
Cancer discovery - 1 Feb 2013
Lee Ho-June, Schaefer Gabriele, Heffron Timothy P, Shao Lily, Ye Xiaofen, Sideris Steve, Malek Shiva, Chan Emily, Merchant Mark, La Hank, Ubhayakar Savita, Yauch Robert L, Pirazzoli Valentina, Politi Katerina, Settleman Jeff
Abstract excerpt
UNLABELLED: Approximately half of EGFR-mutant non-small cell lung cancer (NSCLC) patients treated with small-molecule EGFR kinase inhibitors develop drug resistance associated with the EGF receptor (EGFR) T790M "gatekeeper" substitution, prompting efforts to develop covalent EGFR inhibitors, which can effectively suppress EGFR T790M in preclinical models. However, these inhibitors have yet to prove clinically...
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