Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib

Cancer Research

Volumn 66, Issue 16, 2006, Pages 8163-8171

  Carey, Kendall D ^a   Garton, Andrew J ^b   Romero, Maria S ^a   Kahler, Jennifer ^b   Thomson, Stuart ^b   Ross, Sarajane ^a   Park, Frances ^c   Haley, John D ^b   Gibson, Neil ^b   Sliwkowski, Mark X ^a  

^a GENENTECH INC   (United States)

^b OSI PHARMACEUTICALS INC   (United States)

^c SGX Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; MUTANT PROTEIN; OSI 744;

ANIMAL CELL; ARTICLE; CARCINOGENICITY; CELL CYCLE PROGRESSION; CELL TRANSFORMATION; CONTROLLED STUDY; DRUG MECHANISM; DRUG SENSITIVITY; LUNG NON SMALL CELL CANCER; MOUSE; NONHUMAN; PRIORITY JOURNAL; SOMATIC MUTATION; TUMOR GROWTH;

CELL DIVISION; CELL LINE, TUMOR; CELL TRANSFORMATION, NEOPLASTIC; CLONING, MOLECULAR; GENETIC VECTORS; HUMANS; KINETICS; MUTAGENESIS; MUTATION; PROTEIN KINASE INHIBITORS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; SEQUENCE DELETION;

EID: 33748066632     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-06-0453     Document Type: Article

References (49)

1. Mendelsohn J, Baselga J. The EGF receptor family as targets for cancer therapy. Oncogene 2000;19:6550-65.
2. Mendelsohn J. Antibody-mediated EGF receptor blockade as an anticancer therapy: from the laboratory to the clinic. Cancer Immunol Immunother 2003;52:342-6.
3. Pollack VA, Savage DM, Baker DA, et al. Inhibition of epidermal growth factor receptor-associated tyrosine phosphorylation in human carcinomas with CP-358,774: dynamics of receptor inhibition in situ and antitumor effects in athymic mice. J Pharmacol Exp Ther 1999;291:739-48.
4. Higgins B, Kolinsky K, Smith M, et al. Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models. Anticancer Drugs 2004;15:503-12.
5. Johnson JR, Cohen M, Sridhara R, et al. Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Clin Cancer Res 2005;11:6414-21.
6. Pao W, Miller VA. Epidermal growth factor receptor mutations, small-molecule kinase inhibitors, and non-small-cell lung cancer: current knowledge and future directions. J Clin Oncol 2005;23:2556-68.
7. Johnson BE, Janne PA. Epidermal growth factor receptor mutations in patients with non-small cell lung cancer. Cancer Res 2005;65:7525-9.
8. Lynch TJ, Bell DW, Sordella R, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-39.
9. Paez JG, Janne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 2004;304:1497-500.
10. Huang SF, Liu HP, Li LH, et al. 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 2004;10:8195-203.
11. Han SW, Kim TY, Hwang PG, et al. Predictive and prognostic impact of epidermal growth factor receptor mutation in non-small-cell lung cancer patients treated with gefitinib. J Clin Oncol 2005;23:2493-501.
12. Takano T, Ohe Y, Sakamoto H, et al. Epidermal growth factor receptor gene mutations and increased copy numbers predict gefitinib sensitivity in patients with recurrent non-small-cell lung cancer. J Clin Oncol 2005;23:6829-37.
13. Shigematsu H, Lin L, Takahashi T, et al. Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers. J Natl Cancer Inst 2005;97:339-46.
14. Zhang XT, Li LY, Mu XL, et al. The EGFR mutation and its correlation with response of gefitinib in previously treated Chinese patients with advanced non-small-cell lung cancer. Ann Oncol 2005;16:1334-42.
15. Herbst RS, Prager D, Hermann R, et al. TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. J Clin Oncol 2005;23:5892-9.
16. Shepherd FA, Rodrigues Pereira J, Ciuleanu T, et al. Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med 2005;353:123-32.
17. Tsao MS, Sakurada A, Cutz JC, et al. Erlotinib in lung cancer-molecular and clinical predictors of outcome. N Engl J Med 2005;353:133-44.
18. Eberhard DA, Johnson BE, Amler LC, et al. Mutations in the epidermal growth factor receptor and in KRAS are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib. J Clin Oncol 2005;23:5900-9.
19. Amann J, Kalyankrishna S, Massion PP, et al. Aberrant epidermal growth factor receptor signaling and enhanced sensitivity to EGFR inhibitors in lung cancer. Cancer Res 2005;65:226-35.
20. Hirata A, Hosoi F, Miyagawa M, et al. HER2 overexpression increases sensitivity to gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, through inhibition of HER2/HER3 heterodimer formation in lung cancer cells. Cancer Res 2005;65:4253-60.
21. Thomson S, Buck E, Petti F, et al. Epithelial to mesenchymal transition is a determinant of sensitivity of non-small-cell lung carcinoma cell lines and xenografts to epidermal growth factor receptor inhibition. Cancer Res 2005;65:9455-62.
22. Yauch RL, Januario T, Eberhard DA, et al. Epithelial versus mesenchymal phenotype determines in vitro sensitivity and predicts clinical activity of erlotinib in lung cancer patients. Clin Cancer Res 2005;11:8686-98.
23. Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate antiapoptotic pathways. Science 2004;305:1163-7.
24. Jiang J, Greulich H, Janne PA, Sellers WR, Meyerson M, Griffin JD. 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;65:8968-74.
25. Pao W, Miller V, Zakowski M, et al. 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 2004;101:13306-11.
26. Engelman JA, Janne PA, Mermel C, et al. ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines. Proc Natl Acad Sci U S A 2005;102:3788-93.
27. Chazin VR, Kaleko M, Miller AD, Slamon DJ. Transformation mediated by the human HER-2 gene independent of the epidermal growth factor receptor. Oncogene 1992;7:1859-66.
28. Pruss RM, Herschman HR, Klement V. 3T3 variants lacking receptors for epidermal growth factor are susceptible to transformation by Kirsten sarcoma virus. Nature 1978;274:272-4.
29. Moyer JD, Barbacci EG, Iwata KK, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res 1997;57:4838-48.
30. Gebhardt A, Bell JC, Foulkes JG. Abelson transformed fibroblasts lacking the EGF receptor are not tumourigenic in nude mice. EMBO J 1986;5:2191-5.
31. Wood ER, Truesdale AT, McDonald OB, et al. 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 2004;64:6652-9.
32. Di Fiore PP, Pierce JH, Fleming TP, et al. Overexpression of the human EGF receptor confers an EGF-dependent transformed phenotype to NIH 3T3 cells. Cell 1987;51:1063-70.
33. Velu TJ, Beguinot L, Vass WC, et al. Epidermal-growth-factor-dependent transformation by a human EGF receptor proto-oncogene. Science 1987;238:1408-10.
34. Velu TJ. Structure, function and transforming potential of the epidermal growth factor receptor. Mol Cell Endocrinol 1990;70:205-16.
35. Haley JD, Hsuan JJ, Waterfield MD. Analysis of mammalian fibroblast transformation by normal and mutated human EGF receptors. Oncogene 1989;4:273-83.
36. Okabayashi Y, Kido Y, Okutani T, Sugimoto Y, Sakaguchi K, Kasuga M. Tyrosines 1148 and 1173 of activated human epidermal growth factor receptors are binding sites of She in intact cells. J Biol Chem 1994;269:18674-8.
37. Holgado-Madruga M, Emlet DR, Moscatello DK, Godwin AK, Wong AJ. A Grb2-associated docking protein in EGF- and insulin-receptor signalling. Nature 1996;379:560-4.
38. Stamos J, Sliwkowski MX, Eigenbrot C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J Biol Chem 2002;277:46265-72.
39. Gazdar AF, Shigematsu H, Herz J, Minna JD. Mutations and addiction to EGFR: the Achilles "heal" of lung cancers? Trends Mol Med 2004;10:481-6.
40. Kwak EL, Sordella R, Bell DW, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A 2005;102:7665-70.
41. Ravid T, Heidinger JM, Gee P, Khan EM, Goldkorn T. c-Cbl-mediated ubiquitinylation is required for epidermal growth factor receptor exit from the early endosomes. J Biol Chem 2004;279:37153-62.
42. Grovdal LM, Stang E, Sorkin A, Madshus IH. Direct interaction of Cbl with pTyr 1045 of the EGF receptor (EGFR) is required to sort the EGFR to lysosomes for degradation. Exp Cell Res 2004;300:388-95.
43. Batzer AG, Rotin D, Urena JM, Skolnik EY, Schlessinger J. Hierarchy of binding sites for Grb2 and She on the epidermal growth factor receptor. Mol Cell Biol 1994;14:5192-201.
44. Kakiuchi S, Daigo Y, Ishikawa N, et al. Prediction of sensitivity of advanced non-small cell lung cancers to gefitinib (Iressa, ZD1839). Hum Mol Genet 2004;13:3029-43.
45. Chou TY, Chiu CH, Li LH, et al. Mutation in the tyrosine kinase domain of epidermal growth factor receptor is a predictive and prognostic factor for gefitinib treatment in patients with non-small cell lung cancer. Clin Cancer Res 2005;11:3750-7.
46. Hidalgo M, Bloedow D. Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of Erlotinib (Tarceva). Semin Oncol 2003;30:25-33.
47. Shah NT, Miller VA. Antitumor activity and tolerability of gefitinib in patients with non-small-cell lung cancer treated in an expanded access program. Clin Lung Cancer 2003;5:182-6.
48. Malik SN, Siu LL, Rowinsky EK, et al. Pharmacodynamic evaluation of the epidermal growth factor receptor inhibitor OSI-774 in human epidermis of cancer patients. Clin Cancer Res 2003;9:2478-86.
49. Mohamed MK, Ramalingam S, Lin Y, Gooding W, Belani CP. Skin rash and good performance status predict improved survival with gefitinib in patients with advanced non-small cell lung cancer. Ann Oncol 2005;16:780-5.