Article
Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.
Cancer discovery - 1 Oct 2012
Ercan Dalia, Xu Chunxiao, Yanagita Masahiko, Monast Calixte S, Pratilas Christine A, Montero Joan, Butaney Mohit, Shimamura Takeshi, Sholl Lynette, Ivanova Elena V, Tadi Madhavi, Rogers Andrew, Repellin Claire, Capelletti Marzia, Maertens Ophélia, Goetz Eva M, Letai Anthony, Garraway Levi A, Lazzara Matthew J, Rosen Neal, Gray Nathanael S, Wong Kwok-Kin, Jänne Pasi A
Abstract excerpt
The clinical efficacy of epidermal growth factor receptor (EGFR) kinase inhibitors is limited by the development of drug resistance. The irreversible EGFR kinase inhibitor WZ4002 is effective against the most common mechanism of drug resistance mediated by the EGFR T790M mutation. Here, we show, in multiple complementary models, that resistance to WZ4002 develops through aberrant activation of extracellular...
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