EGFR mutation and resistance of non-small-cell lung cancer to gefitinib.

By Susumu S. Kobayashi, T. Boggon, Tajhal Dayaram, P. Jänne, O. Kocher, Matthew Meyerson, B. Johnson, M. Eck, Daniel G. Tenen, B. Halmos. New England Journal of Medicine, 2005

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Analysis of Epidermal Growth Factor Receptor Gene Mutation in Patients with Non–Small Cell Lung Cancer and Acquired Resistance to Gefitinib (2006, background): “Recently, it has been reported by two groups that a secondary threonine-to-methionine mutation at codon 790 (T790M) of the EGFR gene is related to the acquired resistance to gefitinib and erlotinib (9, 10).”
ERBB receptors: From oncogene discovery to basic science to mechanism-based cancer therapeutics (2014, background): “Intrinsic EGFR Alterations In EGFR mutant lung cancer, the most common mechanism of acquired resistance to EGFR inhibitors is the development of a mutation in the gatekeeper residue of EGFR, T790M (Kobayashi et al., 2005; Pao et al., 2005).”
Mechanisms and insights into drug resistance in cancer (2013, background): “…result of mutations occurring at the gatekeeper residues of the kinase domain which disables drug binding (Gorre et al., 2001; Blencke et al., 2003; Kobayashi et al., 2005; Pao et al., 2005; Soverini et al., 2005; Balak et al., 2006; Jabbour et al., 2006, 2008; Nicolini et al., 2006; Apperley,…”