The epidermal growth factor receptor-L861Q mutation increases kinase activity without leading to enhanced sensitivity toward epidermal growth factor receptor kinase inhibitors

Journal of Thoracic Oncology

Volumn 6, Issue 2, 2011, Pages 387-392

  Kancha, Rama Krishna ^a   Peschel, Christian ^a   Duyster, Justus ^a  

^a TECHNICAL UNIVERSITY OF MUNICH   (Germany)

Author keywords

Drug sensitivity; EGFR; Erlotinib; Gefitinib; Kinase activity

Indexed keywords

6 [4 (4 ETHYL 1 PIPERAZINYLMETHYL)PHENYL] 4 (ALPHA METHYLBENZYLAMINO) 7H PYRROLO[2,3 D]PYRIMIDINE; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; LIGAND; UNCLASSIFIED DRUG; WZ 4002;

ARTICLE; ASSAY; DELETION MUTANT; DRUG SENSITIVITY; ENZYME ACTIVATION; ENZYME ACTIVITY; HUMAN; HUMAN CELL; POINT MUTATION; PRIORITY JOURNAL; PROTEIN DOMAIN; WILD TYPE;

ANIMALS; BLOTTING, WESTERN; CELL PROLIFERATION; DRUG RESISTANCE, NEOPLASM; HUMANS; KIDNEY; MICE; MUTATION; PRECURSOR CELLS, B-LYMPHOID; PROTEIN KINASE INHIBITORS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 79551552012     PISSN: 15560864     EISSN: 15561380     Source Type: Journal    
DOI: 10.1097/JTO.0b013e3182021f3e     Document Type: Article

References (15)

1. Lynch TJ, Bell DW, Sordella R, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of nonsmall-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-2139.
2. Sharma SV, Bell DW, Settleman J, et al. Epidermal growth factor receptor mutations in lung cancer. Nat Rev Cancer 2007;7:169-181.
3. Kobayashi S, Boggon TJ, Dayaram T, et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 2005;352:786-792.
4. Greulich H, Chen TH, Feng W, et al. Oncogenic transformation by inhibitor-sensitive and-resistant EGFR mutants. PLoS Med 2005;2: e313.
5. Kancha RK, von Bubnoff N, Peschel C, et al. Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy. Clin Cancer Res 2009;15:460-467.
6. Lee JC, Vivanco I, Beroukhim R, et al. Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain. PLoS Med 2006;3: e485.
7. Jiang J, Greulich H, Janne PA, et al. Epidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progression. Cancer Res 2005;65:8968-8974.
8. Pedersen MW, Meltorn M, Damstrup L, et al. The type III epidermal growth factor receptor mutation. Biological significance and potential target for anti-cancer therapy. Ann Oncol 2001;12:745-760.
9. Sakai K, Arao T, Shimoyama T, et al. Dimerization and the signal transduction pathway of a small in-frame deletion in the epidermal growth factor receptor. FASEB J 2006;20:311-313.
10. Chen YR, Fu YN, Lin CH, et al. Distinctive activation patterns in constitutively active and gefitinib-sensitive EGFR mutants. Oncogene 2006;25:1205-1215.
11. Yun CH, Boggon TJ, Li Y, et al. Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. Cancer Cell 2007;11:217-227.
12. Carey KD, Garton AJ, Romero MS, et al. Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib. Cancer Res 2006;66:8163-8171.
13. Kancha RK, Grundler R, Peschel C, et al. Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations. Exp Hematol 2007;35:1522-1526.
14. Zhou W, Ercan D, Chen L, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009;462:1070-1074.
15. Zhang Q, Liu Y, Gao F, et al. Discovery of EGFR selective 4, 6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J Am Chem Soc 2006;128:2182-2183.