Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain

PLoS Medicine

Volumn 2, Issue , 2005, Pages 0225-0235

  Pao, William ^a   Miller, Vincent A ^a   Politi, Katerina A ^a   Riely, Gregory J ^a   Somwar, Romel ^a   Zakowski, Maureen F ^a   Kris, Mark G ^a   Varmus, Harold ^a  

^a MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR KINASE; ERLOTINIB; GEFITINIB; IMATINIB; METHIONINE; PACLITAXEL; THREONINE; TRASTUZUMAB; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; QUINAZOLINE DERIVATIVE;

AMINO ACID SEQUENCE; ARTICLE; CANCER RESISTANCE; CASE REPORT; DISEASE ASSOCIATION; EXON; FEMALE; GENE MUTATION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; HUMAN TISSUE; LUNG ADENOCARCINOMA; ONCOGENE; PROTEIN DOMAIN; ADENOCARCINOMA; DISEASE COURSE; DRUG RESISTANCE; GENETICS; LUNG NON SMALL CELL CANCER; LUNG TUMOR; MIDDLE AGED; NUCLEOTIDE SEQUENCE; POINT MUTATION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; TUMOR CELL CULTURE;

ADENOCARCINOMA; ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; DISEASE PROGRESSION; DNA MUTATIONAL ANALYSIS; DRUG RESISTANCE, NEOPLASM; EXONS; FEMALE; HUMANS; LUNG NEOPLASMS; MIDDLE AGED; POINT MUTATION; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; TUMOR CELLS, CULTURED;

EID: 18244371651     PISSN: 15491277     EISSN: None     Source Type: Journal    
DOI: 10.1371/journal.pmed.0020073     Document Type: Article

References (28)

1. Lynch TJ, Bell DW, Sordella R, Gurubhagavatula S, Okimoto RA, et al. (2004) Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 350: 2129-2139.
2. Paez JG, Janne PA, Lee JC, Tracy S, Greulich H, et al. (2004) EGFR mutations in lung cancer: Correlation with clinical response to gefitinib therapy. Science 304: 1497-1500.
3. Pao W, Miller V, Zakowski M, Doherty J, Politi K, et al. (2004) EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A 101: 13306-13311.
4. Huang SF, Liu HP, Li LH, Ku YC, Fu YN, et al. (2004) High frequency of epidermal growth factor receptor mutations with complex patterns in non-small cell lung cancers related to gefitinib responsiveness in Taiwan. Clin Cancer Res 10: 8195-8203.
5. Kosaka T, Yatabe Y, Endoh H, Kuwano H, Takahashi T, et al. (2004) Mutations of the epidermal growth factor receptor gene in lung cancer: Biological and clinical implications. Cancer Res 64: 8919-8923.
6. Shigematsu H, Lin L, Takahashi T, Nomura M, Suzuki M, et al. (2004) Clinical and biological features of epidermal growth factor receptor mutations in lung cancers. J Natl Cancer Inst. In press.
7. Pao W, Wang TY, Riely GJ, Miller VA, Pan Q, et al. (2005) KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Medicine 2: e17.
8. Deininger M, Buchdunger E, Druker BJ (2004) The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood: Epub ahead of print.
9. Al-Ali HK, Heinrich MC, Lange T, Krahl R, Mueller M, et al. (2004) High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib. Hematol J 5: 55-60.
10. Gorre ME, Mohammed M, Ellwood K, Hsu N, Paquette R, et al. (2001) Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 293: 876-880.
11. Shah NP, Nicoll JM, Nagar B, Gorre ME, Paquette RL, et al. (2002) Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2: 117-125.
12. O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, et al. (2004) Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: Implications for CML. Blood 104: 2532-2539.
13. Shah NP, Tran C, Lee FY, Chen P, Norris D, et al. (2004) Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 305: 399-401.
14. Sawyers C (2004) Targeted cancer therapy. Nature 432: 294-297.
15. Tamborini E, Bonadiman L, Greco A, Albertini V, Negri T, et al. (2004) A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient. Gastroenterology 127: 294-299.
16. Cools J, DeAngelo DJ, Gotlib J, Stover EH, Legare RD, et al. (2003) A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome. N Engl J Med 348: 1201-1214.
17. Krug LM, Miller VA, Crapanzano J, Ng KK, Pizzo B, et al. (2001) Randomized phase II trial of trastuzumab (tras) plus either weekly docetaxel (doc) or paclitaxel (pac) in previously untreated advanced non-small cell lung cancer (NSCLC). Proc Am Soc Clin Oncol 20: 1328.
18. Sordella R, Bell DW, Haber DA, Settleman J (2004) Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 305: 1163-1167.
19. Tracy S, Mukohara T, Hansen M, Meyerson M, Johnson BE, et al. (2004) Gefitinib induces apoptosis in the EGFRL858R non-small cell lung cancer cell line H3255. Cancer Res 64: 7241-7244.
20. Bozyczko-Coyne D, McKenna BW, Connors TJ, Neff NT (1993) A rapid fluorometric assay to measure neuronal survival in vitro. J Neuroscience Meth 50: 205-216.
21. Blencke S, Zech B, Engkvist O, Greff Z, Orfi L, et al. (2004) Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors. Chem Biol 11: 691-701.
22. Blencke S, Ullrich A, Daub H (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: 15435-15440.
23. Kreuzer KA, Le Coutre P, Landt O, Na IK, Schwarz M, et al. (2003) Preexistence and evolution of imatinib mesylate-resistant clones in chronic myelogenous leukemia detected by a PNA-based PCR clamping technique. Ann Hematol 82: 284-289.
24. Stamos J, Sliwkowski MX, Eigenbrot C (2002) Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J Biol Chem 277: 46265-46272.
25. Daub H, Specht K, Ullrich A (2004) Strategies to overcome resistance to targeted protein kinase inhibitors. Nat Rev Cancer 3: 1001-1010.
26. Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, et al. (2004) A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 64: 6652-6659.
27. Chen LL, Trent JC, Wu EF, Fuller GN, Ramdas L, et al. (2004) A missense mutation in KIT kinase domain 1 correlates with imatinib resistance in gastrointestinal stromal tumors. Cancer Res 64: 5913-5919.
28. Gorre ME, Sawyers CL (2002) Molecular mechanisms of resistance to STI571 in chronic myeloid leukemia. Curr Opin Hematol 9: 303-307.