Epidermal growth factor receptor (EGFR) and EGFR mutations, function and possible role in clinical trials

Annals of Oncology

Volumn 8, Issue 12, 1997, Pages 1197-1206

  Rude Voldborg, B ^a   Damstrup, L ^a   Spang Thomsen, M ^b   Skovgaard Poulsen, H ^a  

^a FINSEN LABORATORY   (Denmark)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Cancer; Epidermal growth factor receptor; Signalling; Tyrosine kinase

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR; PROTEIN TYROSINE KINASE;

CELL DIFFERENTIATION; CELL PROLIFERATION; DNA SYNTHESIS; GENE DELETION; GENE MUTATION; LIGAND BINDING; MUTATION; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION;

CLINICAL TRIALS; GENE DELETION; HUMANS; MUTATION; NEOPLASMS; PHENOTYPE; RECEPTOR, EPIDERMAL GROWTH FACTOR; SIGNAL TRANSDUCTION;

EID: 7144227965     PISSN: 09237534     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1008209720526     Document Type: Review

References (100)

1. Cohen S. The epidermal growth factor (EGF). Cancer 1983; 51: 1787-91.
2. Yarden Y, Schlessinger J. Epidermal growth factor induces rapid reversible aggregation of the purified epidermal growth factor receptor. Biochemistry 1987; 26: 1443-51.
3. Hsuan JJ. Oncogene regulation by growth factors. Anticancer Res. 1993; 13: 2521-2.
4. Soler C, Beguinot L, Carpenter G. Individual epidermal growth factor receptor autophosphorylation sites do not stringently define association motifs for several SH-2 containing proteins. J Biol Chem 1994; 269: 12320-4.
5. Margolis B, Li N, Koch A et al. The tyrosine phosphorylated carboxyterminus of the EGF receptor is a binding site for GAP and PLC-gamma. EMBO J. 1990; 9: 4375-80.
6. Anderson D, Koch CA, Grey L et al. Binding of SH2 domains of phospholipase C gamma 1, GAP, and Src to activated growth factor receptors. Science 1990; 250: 979-2.
7. Nishibe S, Wahl MI, Hernandez-Sotomajor SMT et al. Increase of the catalytic activity of phospholipase C-gamma 1 by tyrosine phosphorylation. Science 1990; 243: 1553-6.
8. Gill GN. Regulation of EGF receptor expression and function. Molecular Reproduction and Development 1990; 27: 46-53.
9. French AR, Sudlow GP. Wiley HS et al. Postendocytotic trafficking of epidermal growth factor-receptor complexes is mediated through saturable and specific endosomal interactions. J Biol Chem 1994; 269: 15749-55.
10. Carpenter G, Cohen S. Epidermal growth factor. J Biol Chem 1990; 265: 7709-12.
11. Marquardt H, Hunkapiller MW, Hood LE et al. Transforming growth factors produced by retrovirus transformed rodent fibroblasts and human melanoma cells: Amino acid homology with epidermal growth factor. Proc Natl Acad Sci USA 1983: 4684-8.
12. Shoyab M, McDonald VL, Bradley JF et al. Amphiregulin: a bifunctional growth-modulating glycoprotein produced by the phorbol 12-myristate 13-acetate-treated human breast adenocarcinoma cell line MCF-7. Proc Natl Acad Sci USA 1988; 85: 6528-32.
13. Shing Y, Christofori G, Hanahan D et al. Betacellulin: a mitogen from pancreatic b-cell tumors. Science 1993; 259: 1604-7.
14. Ekstrand AJ, Sugawa N, James CD et al. Amplified and rearranged epidermal growth factor receptor genes in human glioblastomas reveal deletions of sequences encoding portions of the N- and/or C-terminal tails. Proc Natl Acad Sci USA 1992; 89: 4309-13.
15. Garcia de Pallazzo I, Adams GP, Sundareshan P et al. Expression of mutated epidermal growth factor receptor by non-small cell lung carcinomas. Cancer Res 1993; 53: 3217-20.
16. Wikstrand CJ, Hale LP, Batra KS et al. Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomas. Cancer Res 1995; 55: 3140-8.
17. Moscatello DK, Holgado-Madruga M, Godwin AK et al. Frequent expression of a mutant epidermal growth factor receptor in multiple human tumors. Cancer Res 1995; 55: 5536-9.
18. Sugawa N, Ekstrand AJ, James CD et al. Identical splicing of aberrant epidermal growth factor receptor transcripts from amplified rearranged genes in human glioblastomas. Proc Natl Acad Sci USA 1990; 87: 8602-6.
19. Bigner SH, Humphrey PA, Wong AJ et al. Characterization of the epidermal growth factor receptor in human glioma cell lines and xenografts. Cancer Res 1990; 50: 8013-7.
20. Humphrey PA, Wong AJ, Vogelstein B et al. Amplification and expression of the epidermal growth factor receptor gene in human glioma xenografts. Cancer Res 1988; 48: 2231-8.
21. Kris RM, Lax I, Gullick WJ et al. Anibodies against a synthetic peptide as a probe for the kinase activity of the avian EGF receptor and v-erb B protein. Cell 1985; 40: 619-25.
22. Gilmore T, Declue JE, Martin GS. Protein phosphorylation at tyrosine is induced by the r-erb B gene product in vivo and in vitro. Cell 1985; 40: 609-18.
23. Humphrey PA, Gangarosa LM, Wong AJ et al. Deletion-mutant epidermal growth factor receptor in human gliomas: Effect of type II mutation on receptor function. Biochem Biophys Res Comm 1991; 178: 1413-20.
24. Yamazaki H, Ohba Y, Tamaoki N et al. A deletion mutation within the ligand binding domain is responsible for activation of epidermal growth factor gene in human brain tumors. Jpn J Cancer Res 1990; 81: 773-9.
25. Wong AJ, Ruppert JM, Bigner SH et al. Structural alterations of the epidermal growth factor receptor gene in human gliomas. Proc Natl Acad Sci USA 1992; 89: 2965-9.
26. Humphrey PA, Wong AJ, Vogelstein B et al. Anti-synthetic peptide antibody reacting at the fusion junction of deletion-mutant epidermal growth factor receptors in human glioblastoma. Proc Natl Acad Sci USA 1990; 87: 4207-11.
27. Ekstrand AJ, Longo N, Hamid ML et al. Functional characterization of an EGF receptor with a truncated extracellular domain expressed in glioblastomas with EGFR gene amplification. Oncogene 1994; 9; 2313-20.
28. Nishikawa R, Xiang-Dong J, Harmon RC et al. A mutant epidermal growth factor receptor common in human glioma confers enhanced tumorigenicity. Proc Natl Acad Sci USA 1994; 91: 7727-31.
29. Huang H-JS, Nagane M, Klingbeil CK et al. The enhanced tumorigenic activity of a mutant epidermal growth factor receptor common in human cancers is mediated by threshold levels of constitutive tyrosine phosphorylation and unattenuated signalling. J Biol Chem 1997; 272: 2927-35.
30. Lorimer IAJ, Wikstrand CJ, Batra SK et al. Immunotoxins that target an oncogenic mutant epidermal growth factor receptor expressed in human tumors. Clin Cancer Res 1995; 1: 859-64.
31. Hills D, Rowlinson Busza G, Gullick WJ. Specific targeting of a mutant, activated EGF receptor found in glioblastoma using a monoclonal antibody. Int J Cancer 1995; 63: 537-43.
32. Ekstrand AJ, Liu L, He J et al. Altered subcellular location of an activated and tumor-associated epidermal growth factor receptor. Oncogene 1995; 10: 1455-60.
33. Savage CRJ, Hash JH, Cohen S. Epidermal growth factor. J Biol Chem 1973; 248: 7669-72.
34. Johnson GR, Wong L. Heparin sulfate is essential to amphiregulin.induced mitogenic signaling by the epidermal growth factor receptor. J Biol Chem 1994; 269: 27149-54.
35. Besner GE, Whelton D, Crissman-Combs MA et al. Modulation of heparin-binding EGF-like growth factor (HB-EGF), with the epidermal growth factor receptor: Modulation by heparin, heparinase or synthetic heparin-binding HB-EGF fragments. Growth Factors 1992; 7: 289-96.
36. Prigent SA, Lemoine NR. The type 1 (EGFr-related) family of growth factor receptors and their ligands. Prog in Growth Factor Res 1992; 4: 1-24.
37. Earp HS, Dawson TL, Li X et al. Heterodimerization and functional interaction between EGF receptor family members: A new signaling paradigm with implications for breast cancer research. Breast Cancer Res Treat 1995; 35: 115-32.
38. Wang Z, Moran MF. Requirement for the adapter protein GRB2 in EGF receptor endocytosis. Science 1996; 272: 1935-39.
39. Cochet C, Gill GN, Meisenhelder J et al. C-kinase phosphorylates the epidermal growth factor receptor and reduces its epidermal growth factor-stimulated tyrosine protein kinase activity. J Biol Chem 1984; 259: 2553-8.
40. Downward J, Waterfield MD, Parker PJ. Autophosphorylation and protein kinase C phosphorylation of the epidermal growth factor receptor. J Biol Chem 1985; 260: 14538-46.
41. Friedman HS, Frackelton AR, Ross AH et al. Tumor promoters block tyrosine-specific phosphorylation of the epidermal growth factor receptor. Proc Natl Acad Sci USA 1984; 81: 3034-8.
42. Wiley HS, Herbst JJ, Walsh BJ et al. The role of tyrosine kinase activity in endocytosis, compartmentation, and down-regulation of the epidermal growth factor receptor. J Biol Chem 1991; 266: 11083-94.
43. Opresko LK, Chang CP, Will BH et al. Endocytosis and lysosomal targeting of epidermal growth factor receptors are mediated by distinct sequences independent of the tyrosine kinase domain. J Biol Chem 1995; 270: 4325-33.
44. Chen WS, Lazar CS, Lund KA et al. Functional independence of the epidermal growth factor receptor from a domain required for ligand-induced internalization and calcium regulation. Cell 1989; 59: 33-43.
45. Schuh SM, Newberry EP, Dalton MA et al. Mutation of proline-1003 to glycine in the epidermal growth factor (EGF) receptor enhances responsiveness to EGF. Mol Biol Cell 1994; 5: 739-46.
46. Ullrich A, Schlessinger J. Signal transduction by receptors with tyrosine kinase activity. Cell 1990; 61: 203-12.
47. Nishizuka Y. The molecular heterogeneity of protein kinase C and its implications for cellular regulation. Nature 1988; 334: 661-8.
48. Molloy CJ, Bottaro DP, Fleming TP et al. PDGF induction of tyrosine phosphorylation of GTPase activating protein. Nature 1989; 342: 711-4.
49. Boguski MS, McCormick F. Proteins regulating Ras and its relatives. Nature 1993; 366: 643-54.
50. Howe LR, Leevers SJ, Gomez N et al. Activation of the MAP kinase pathway by the protein kinase raf. Cell 1992; 71: 335-42.
51. Davis RJ. The mitogen-activated protein kinase signal transduction pathway. J Biol Chem 1993; 268: 14553-6.
52. Hunter T. Oncoprotein networks. Cell 1997; 88: 333-46.
53. Hunter T, Pines J. Cyclins and cancer. II: cyclin D and ADK inhibitors come of age. Cell 1994; 79: 573-82.
54. 1 arrest mediated by anti-epidermal growth factor receptor monoclonal antibody. Oncogene 1996; 12: 1397-1403.
55. Sommers CL, Gelman EP, Kemler R et al. Alterations in b-catenin phosphyrolation and plakoglobin expression in human breast cancer cells. Cancer Res 1994; 54: 3544-52.
56. Wilding J, Vousden KH, Soutter WP et al. E-cadherin transfection down-regulates the epidermal growth factor receptor and reverses the invasive phenotype of human papilloma virus-transfected keratinocytes. Cancer Res 1996; 56: 5285-92.
57. Wang Z, Tung PS, Moran MF. Association of P120 Ras Gap with endocytic components and colocalization with epidermal growth factor (EGF) receptor in response to EGF stimulation. Cell Growth Diff. 1996; 7: 123-33.
58. Libermann TA, Nusbaum HR, Razon N et al. Amplification, enhanced expression and possible rearrangement of EGF receptor gene in primary human brain tumours of glial origin. Nature 1985; 313: 144-7.
59. Sauter G, Maeda T, Waldman FM et al. Patterns of epidermal growth factor receptor amplification in malignant gliomas. Am J Pathol 1996; 148: 1047-53.
60. Xu Y, Richert N, Ito S et al. Characterization of epidermal growth factor receptor gene expression in malignant and normal human cell lines. Proc Natl Acad Sci USA 1984; 81: 7308-12.
61. Harris AL, Nicholson S, Sainsbury R et al. Epidermal growth factor receptor and other oncogenes as prognostic markers. J Natl Cancer Inst Monogr 1992; 11: 181-7.
62. Shiozaki H, Kadowaki T, Doki Y et al. Effect of epidermal growth factor on cadherin-mediated adhesion in a human oesophageal cancer cell line. Br J Cancer 1995; 71: 250-8.
63. Davies DE, Chamberlin SG. Targeting the epidermal growth factor receptor for therapy of carcinomas. Biochem Biophys Res Comm 1996; 51: 1101-10.
64. Diedrich U, Lucius J, Baron E et al. Distribution of epidermal growth factor receptor gene amplification in brain tumours and correlation to prognosis. J Neurol 1995; 242: 683-8.
65. Kitagawa Y, Ueda M, Ando N et al. Further evidence for prognostic significance of epidermal growth factor receptor gene amplification in patients with esophageal squamous cell carcinoma. Clin Cancer Res 1996; 2: 909-14.
66. Maurizi M, Scambia G, Benedetti Panici P et al. EGF receptor expression in primary laryngeal cancer: correlation with clinicopathological features and prognostic significance. Int J Cancer 1992; 52: 862-6.
67. Fujino S, Enokibori T, Tezuka N et al. A comparison of epidermal growth factor receptor levels and other prognostic parameters in non-small cell lung cancer. Eur J Cancer 1996; 32A: 2070-4.
68. Pfeiffer P, Clausen PP, Andersen K et al. Lack of prognostic significance of epidermal growth factor receptor and the oncoprotein p185HER-2 in patients with systemically untreated non-small-cell lung cancer: An immunohistochemical study on cryo-sections. Br J Cancer 1996; 74: 86-91.
69. Veale D, Kerr N, Gibson GJ et al. The relationship of quantitave epidermal growth factor receptor expression in non-small-cell lung cancer to long term survival. Br J Cancer 1993; 68: 162-5.
70. Dazzi H, Hasleton PS, Thatcher N et al. Expression of epidermal growth factor receptor (EGF-R) in non-small cell lung cancer. Use of archival tissue and correlation of EGF-R with histology, tumour size, node status and survival. Br J Cancer 1989; 59: 746-9.
71. Veale D, Ashcroft T, Marsh C et al. Epidermal growth factor receptors in non-small-cell lung cancer. Br J Cancer 1987; 55: 513-6.
72. 1. Cancer Res 1996; 56: 3666-9.
73. Modjtahedi H, Eccles SA, Sandle J et al. Differentation or immune destruction: Two pathways for therapy of squamos cell carcinomas with antibodies to the epidermal growth factor receptor. Cancer Res 1994; 54: 1695-1701.
74. Normanno N, Bianco C, Damiano V et al. Growth inhibition of human colon carcinoma cells by combinations of anti-epidermal growth factor-related growth factor antisense oligonucleotides. Clin Cancer Res 1996; 2: 601-9.
75. Moroni MC, Willingham MC, Beguinot L. EGF-R antisense RNA blocks expression of the epidermal growth factor receptor and supresses the transforming phenotype of a human carcinoma cell line. J Biol Chem 1992; 267: 2714-22.
76. Arteaga CL, Hurd SD, Dugger TC et al. Epidermal growth factor receptors in human breast carcinoma cells: A potential selective target for transforming growth factor a-Pseudonomas exotoxin 40 fusion protein. Cancer Res 1996; 54: 4703-9.
77. Qian X, Dougall WC, Hellman ME et al. Kinase-deficient neu proteins suppress epidermal growth factor receptor function and abolish cell transformation. Oncogene 1994; 9: 1507-14.
78. Honegger AM, Schmidt A, Ullrich A et al. Evidence for epidermal growth factor (EGF)-induced intermolecular autophosphorylation of the EGF receptors in living cells. Mol Cell Biol 1990; 10: 4035-44.
79. Kashles O, Yarden Y, Fischer R et al. A dominant negative mutation supresses the function of normal epidermal growth factor receptors by heterodimerization. Mol Biol Cell 1991; 11: 1454-63.
80. Orourke DM, Qian XL, Zhang HT et al. Trans receptor inhibition of human glioblastome cells by erbB family ectodomains. Proc Natl Acad Sci USA 1997; 94: 3250-5.
81. Kelloff GJ, Fay JR, Steele VE et al. Epidermal growth factor receptor tyrosine kinase inhibitors as potential cancer chemo-preventives. Cancer Epidemiol Biomarkers Prev 1996; 5: 657-66.
82. Kondapaka BS, Reddy KB. Tyrosine kinase inhibitor as a novel signal transduction and antiproliferative agent: prostate cancer. Mol Cell Endo 1996; 117: 53-8.
83. Reddy KB, Mangold GL, Tandon AK et al. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res 1992; 52: 3636-41.
84. Brunton VG, Kellanf LR, Lear MJ et al. Synthesis and biological evaluation of a series of tyrphostins containing nitrothiophene moieties as possible epidermal growth factor receptor tyrosine kinase inhibitors. Anti cancer drug design 1996; 11: 265-95.
85. Traxler PM, Furet P, Mett H et al. 4-(Phenylamino)pyrrolo-pyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase. J Med Chem 1996; 39: 2285-92.
86. Nelson JM, Fry DW. Cytoskeletal and morphological changes associated with the specific suppression of the epidermal growth factor receptor tyrosine kinase activity in A431 human epidermoid carcinoma. Exp Cell Res 1997; 233: 383-90.
87. Dinney CPN, Parker C, Dong ZY et al. Therapy of human transitional cell carcinoma of the bladder by oral administration of the epidermal growth factor receptor protein tyrosine kinase hibitor 4,5 dianilinophthalimide. Clin Cancer Res 1997; 3: 161-8.
88. Buchdunger E, Mett H, Trinks U et al. 4.5 bis(4 fluoroanilino)-phthalimide: a selective inhibitor of the epidermal growth factor receptor signal transduction pathway with potent in vivo antitumor activity. Clin Cancer Res 1995; 1: 813-21.
89. Kunkel MW, Hook KE, Howard CT et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs 1995; 13: 295-302.
90. Yaish P, Gazit A, Gilon C et al. Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors. Science 1988; 242: 933-5.
91. Lyall RM, Zilberstein A, Gazit A et al. Tyrphostins inhibit epidermal growth factor (EGF)-receptor tyrosine kinase activity in living cells and EGF-stimulated cell proliferation. J Biol Chem 1989; 264: 14503-9.
92. Levitzki A. Tyrphostins-potential antiproliferative agents and novel molecular tools. Biochem Pharmacol 1990; 40: 913-8.
93. Trinks U, Buchdunger E, Furet P et al. Dianilinophthalimides. potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. J Med Chem 1994; 37: 1015-27.
94. Buchdunger E.Trinks U, Mett H et al. 4,5-Dianilinophthalimide: a protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity. Proc Natl Acad Sci USA 1994; 91: 2334-8.
95. 131I-labeled epidermal growth factor. Clin Cancer Res 1996; 2: 13-20.
96. Faillot T, Magdelénat H, Mady E et al. A phase I study of an anti-epidermal growth factor receptor monoclonal antibody for e treatment of malignant gliomas. Neurosurgery 1996; 39: 478-83.
97. Kalofonos HP, Pawlikowska TR, Hemmingway A et al. Antibody guided diagnosis and therapy of brain gliomas using radio-labeled monoclonal antibodies against epidermal growth factor receptor and placental alkaline phosphatase. J Nucl Med 1989; 30: 1636-45.
98. Brady LW, Miyamoto C, Woo DV et al. Malignant astrocytomas treated with iodine-125 labeled monoclonal antibody 425 against epidermal growth factor receptor: A phase II trial. Int J Radiat Oncol Biol Phys 1991; 22: 225-30.
99. Ciardiello F, Damiano V, Bianco R et al. Antitumor activity of combined blockade of epidermal growth factor receptor and protein kinase A J Natl Cancer Inst 1996; 88: 1770-6.
100. Han Y, Caday CG, Nanda A et al. Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors. Cancer Res 1996; 56: 3859-61.