EGFR T790M Mutation: A Double Role in Lung Cancer Cell Survival?

Lynch, 2004, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib, N Engl J Med, 350, 2129, 10.1056/NEJMoa040938 Paez, 2004, EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy, Science, 304, 1497, 10.1126/science.1099314 Mitsudomi, 2007, Mutations of the epidermal growth factor receptor gene and related genes as determinants of epidermal growth factor receptor tyrosine kinase inhibitors sensitivity in lung cancer, Cancer Sci, 98, 1817, 10.1111/j.1349-7006.2007.00607.x Morita, 2008, Gefitinib combined survival analysis of the mutation positives from the prospective phase II trials (I-CAMP), J Clin Oncol, 26, 10.1200/jco.2008.26.15_suppl.8101 Kobayashi, 2005, EGFR mutation and resistance of non-small-cell lung cancer to gefitinib, N Engl J Med, 352, 786, 10.1056/NEJMoa044238 Pao, 2005, Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain, PLoS Med, 2, e73, 10.1371/journal.pmed.0020073 Hynes, 2005, ERBB receptors and cancer: the complexity of targeted inhibitors, Nat Rev Cancer, 5, 341, 10.1038/nrc1609 Yarden, 2001, Untangling the ErbB signalling network, Nat Rev Mol Cell Biol, 2, 127, 10.1038/35052073 Weinstein, 2008, Oncogene addiction, Cancer Res, 68, 3077, 10.1158/0008-5472.CAN-07-3293 Gazdar, 2004, Mutations and addiction to EGFR: the Achilles ‘heal’ of lung cancers?, Trends Mol Med, 10, 481, 10.1016/j.molmed.2004.08.008 Engelman, 2005, ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines, Proc Natl Acad Sci U S A, 102, 3788, 10.1073/pnas.0409773102 Karaman, 2008, A quantitative analysis of kinase inhibitor selectivity, Nat Biotechnol, 26, 127, 10.1038/nbt1358 Gorre, 2002, BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90, Blood, 100, 3041, 10.1182/blood-2002-05-1361 Blencke, 2003, Mutation of threonine 766 in the epidermal growth factor receptor reveals a hotspot for resistance formation against selective tyrosine kinase inhibitors, J Biol Chem, 278, 15435, 10.1074/jbc.M211158200 Balak, 2006, Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors, Clin Cancer Res, 12, 6494, 10.1158/1078-0432.CCR-06-1570 Kosaka, 2006, Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib, Clin Cancer Res, 12, 5764, 10.1158/1078-0432.CCR-06-0714 Nomura, 2007, Polymorphisms, mutations, and amplification of the EGFR gene in non-small cell lung cancers, PLoS Med, 4, 715, 10.1371/journal.pmed.0040125 Yun, 2008, The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP, Proc Natl Acad Sci U S A, 105, 2070, 10.1073/pnas.0709662105 Toyooka, 2005, EGFR mutation and response of lung cancer to gefitinib, N Engl J Med, 352, 2136, 10.1056/NEJM200505193522019 Bell, 2005, Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR, Nat Genet, 37, 1315, 10.1038/ng1671 Vikis, 2007, EGFR-T790M is a rare lung cancer susceptibility allele with enhanced kinase activity, Cancer Res, 67, 4665, 10.1158/0008-5472.CAN-07-0217 Mulloy, 2007, Epidermal growth factor receptor mutants from human lung cancers exhibit enhanced catalytic activity and increased sensitivity to gefitinib, Cancer Res, 67, 2325, 10.1158/0008-5472.CAN-06-4293 Regales, 2007, Development of new mouse lung tumor models expressing EGFR T790M mutants associated with clinical resistance to kinase inhibitors, PLoS ONE, 2, e810, 10.1371/journal.pone.0000810 Li, 2008, BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models, Oncogene, 27, 4702, 10.1038/onc.2008.109 Engelman, 2007, PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib, Cancer Res, 67, 11924, 10.1158/0008-5472.CAN-07-1885 Li, 2007, Bronchial and peripheral murine lung carcinomas induced by T790M-L858R mutant EGFR respond to HKI-272 and rapamycin combination therapy, Cancer Cell, 12, 81, 10.1016/j.ccr.2007.06.005 Gendreau, 2007, Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647, Clin Cancer Res, 13, 3713, 10.1158/1078-0432.CCR-06-2590 Godin-Heymann, 2008, The T790M “gatekeeper” mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor, Mol Cancer Ther, 7, 874, 10.1158/1535-7163.MCT-07-2387 Shimamura, 2005, Epidermal growth factor receptors harboring kinase domain mutations associate with the heat shock protein 90 chaperone and are destabilized following exposure to geldanamycins, Cancer Res, 65, 6401, 10.1158/0008-5472.CAN-05-0933 Apperley, 2007, Part I: mechanisms of resistance to imatinib in chronic myeloid leukaemia, Lancet Oncol, 8, 1018, 10.1016/S1470-2045(07)70342-X Costa, 2007, BIM mediates EGFR tyrosine kinase inhibitor-induced apoptosis in lung cancers with oncogenic EGFR mutations, PLoS Med, 4, 1669, 10.1371/journal.pmed.0040315 Engelman, 2007, MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling, Science, 316, 1039, 10.1126/science.1141478 Bean, 2007, MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib, Proc Natl Acad Sci U S A, 104, 20932, 10.1073/pnas.0710370104 Guix, 2008, Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins, J Clin Invest, 118, 2609 Zhang, 2006, An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor, Cell, 125, 1137, 10.1016/j.cell.2006.05.013 Yun, 2007, Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity, Cancer Cell, 11, 217, 10.1016/j.ccr.2006.12.017