Epidermal growth factor receptor tyrosine kinase inhibitors as potential cancer chemopreventives

Cancer Epidemiology Biomarkers and Prevention

Volumn 5, Issue 8, 1996, Pages 657-666

  Kelloff, Gary J ^a   Fay, Judith R ^b   Steele, Vernon E ^a   Lubet, Ronald A ^a   Boone, Charles W ^a   Crowell, James A ^a   Sigman, Caroline C ^b  

^a NATIONAL CANCER INSTITUTE   (United States)

^b CCS Associates   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BENZYLIDENE DERIVATIVE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE; FLAVONE DERIVATIVE; LACTONE DERIVATIVE; MALONONITRILE; PHTHALIDE DERIVATIVE; PROTEIN TYROSINE KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; QUINAZOLINE DERIVATIVE; TYROSINE DERIVATIVE;

ANTINEOPLASTIC ACTIVITY; CANCER INHIBITION; CANCER PREVENTION; CHEMOPROPHYLAXIS; DRUG EFFECT; DRUG SCREENING; ENZYME INHIBITION; MALIGNANT NEOPLASTIC DISEASE; NONHUMAN; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; ANTICARCINOGENIC AGENTS; CHEMOPREVENTION; HUMANS; NEOPLASMS; PROTEIN-TYROSINE KINASES; RECEPTOR, EPIDERMAL GROWTH FACTOR; SIGNAL TRANSDUCTION; TRANSFORMING GROWTH FACTOR ALPHA;

EID: 0029833451     PISSN: 10559965     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (108)

1. Kelloff, G. J., Boone, C. W., Crowell, J. A., Steele, V. E., Lubet, R., and Sigman, C. C. Chemopreventive drug development: perspectives and progress. Cancer Epidemiol., Biomarkers & Prev., 3: 85-98.
2. Kelloff, G. J., Boone, C. W., Steele, V. E., Fay, J. R., Lubet, R. A., Crowell, J. A., and Sigman, C. C. Mechanistic considerations in chemopreventive drug development. J. Cell. Biochem., Suppl., 20: 1-24, 1994.
3. Kelloff, G. J., Boone, C. W., Steele, V. E., Fay, J. R., and Sigman, C. C. Inhibition of chemical carcinogenesis. In: J. Arcos, M. Argus, and Y. Woo (eds.), Chemical Induction of Cancer: Modulation and Combination Effects, pp. 73-122. Boston: Birkhäuser Boston, Inc., 1995.
4. Karin, M., and Hunter, T. Transcriptional control by protein phosphorylation: signal transmission from the cell surface to the nucleus. Curr. Biol., 5: 747-757, 1995.
5. Hill, C. S., and Treisman, R. Transcriptional regulation by extracellular signals: mechanisms and specificity. Cell, 80: 199-211, 1995.
6. Cooper, G. M. Oncogenes and growth factors. In: Oncogenes, Chap. 11, pp. 163-173, Boston: Jones and Bartlett Publishers, 1990.
7. Chang, C-J., and Geahlen, R. L. Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J. Nat. Prod. (Lloydia), 55: 1529-1560, 1992.
8. Powis, G. Signalling pathways as targets for anticancer drug development. Pharmacol. & Ther., 62: 57-95, 1994.
9. Powis, G., and Workman, P. Signalling targets for the development of cancer drugs. Anti-Cancer Drug Des., 9: 263-277, 1994.
10. Levitzki, A., and Gazit, A. Tyrosine kinase inhibition: an approach to drug development. Science (Washington DC), 267: 1782-1788, 1995.
11. Shin, D. M., Ro, J. Y., Hong, W. K., and Hittelman, W. N. Dysregulation of epidermal growth factor receptor expression in premalignant lesions during head and neck tumorigenesis. Cancer Res., 54: 3153-3159, 1994.
12. Levitzki, A. Signal-transduction therapy. A novel approach to disease management. Eur. J. Biochem., 226: 1-13, 1994.
13. Gullick, W. J. Prevalence of aberrant expression of the epidermal growth factor receptors in human cancers. Br. Med. Bull., 47: 87-98, 1991.
14. Salomon, D. S., Brandt, R., Ciardiello, F., and Normanno, N. Epidermal growth factor-related peptides and their receptors in human malignancies. Crit. Rev. Oncol. Hematol., 19: 183-232, 1995.
15. Kumar, V., Bustin, S. A., and McKay, I. A. Transforming growth factor α. Cell Biol. Int., 19: 373-388, 1995.
16. Lee, D. C., Fenton, S. E., Berkowitz, E. A., and Hissong, M. A. Transforming growth factor α: expression, regulation, and biological activities. Pharmacol. Rev., 47: 51-85, 1995.
17. Salomon, D. S., Normanno, N., Ciardiello, F., Brandt, R., Shoyab, M., and Todaro, G. J. The role of amphiregulin in breast cancer. Breast Cancer Res. Treat., 33: 103-114, 1995.
18. Boonstra, J., Rijken, P., Humbel, B., Cremers, F., Verkleij, A., and van Bergen-Henegouwen, P. The epidermal growth factor. Cell Biol. Int., 19: 413-430, 1995.
19. Malarkey, K., Belham, C. M., Paul, A., Graham, A., McLees, A., Scott, P. H., and Plevin, R. The regulation of tyrosine kinase signalling pathways by growth factor and G-protein-coupled receptors. Biochem. J., 309: 361-375, 1995.
20. Briscoe, J., Guschin, D., and Muller, M. Just another signalling pathway. Curr. Biol., 4: 1033-1035, 1994.
21. Ekstrand, A. J., Longo, N., Hamid, M. L., Olson, J. L., Liu, L., Collins, V. P., and James, C. D. Functional characterization of an EGF receptor with a truncated extracellular domain expressed in glioblastomas with EGFR gene amplification. Oncogene, 9: 2313-2320, 1994.
22. Ekstrand, A. J., Liu, L., He, J., Hamid, M. L., Longo, N., Collins, V. P., and James, C. D. Altered subcellular location of an activated and tumour-associated epidermal growth factor receptor. Oncogene, 10: 1455-1460, 1995.
23. Nishikawa, R., Ji, X-D., Harmon, R. C., Lazar, C. S., Gill, G. N., Cavenee, W. K., and Huang, H-J. S. A mutant epidermal growth factor receptor common in human glioma confers enhanced tumorigenicity. Proc. Natl. Acad. Sci. USA, 91: 7727-7731.
24. Garcia de Palazzo, I. E., Adams, G. P., Sundareshan, P., Wong, A. J., Testa, J. R., Bigner, D. D., and Weiner, L. M. Expression of mutated epidermal growth factor receptor by non-small cell lung carcinomas. Cancer Res., 53: 3217-3220, 1993.
25. Wikstrand, C. J., Hale, L. P., Batra, S. K., Hill, M. L., Humphrey, P. A., Kurpad, S. N., McLendon, R. E., Mostacello, D., Pegram, C. N., Reist, C. J., Traweek, S. T., Wong, A. J., Zalutsky, M. R., and Bigner, D. D. Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomas. Cancer Res., 55: 3140-3148, 1995.
26. Moscatello, D. K., Holgado-Madruga, M., Godwin, A. K., Ramirez, G., Gunn, G., Zoltick, P. W., Biegel, J. A., Hayes, R. L., and Wong, A. J. Frequent expression of a mutant epidermal growth factor receptor in multiple human tumors. Cancer Res., 55: 5536-5539, 1995.
27. Carter, T. H., and Kung, H. J. Tissue-specific transformation by oncogenic mutants of epidermal growth factor receptor. Crit. Rev. Oncog., 5: 389-428, 1994.
28. Soler, C., Alvarez, C. V., Beguinot, L., and Carpenter, G. Potent SUC tyrosine phosphorylation by epidermal growth factor at low receptor density or in the absence of receptor autophosphorylation sites. Oncogene, 9: 2207-2215, 1994.
29. Jhappan, C., Stahle, C., Harkins, R. N., Fausto, N., Smith, G. H., and Merlino, G. T. TGFα overexpression in transgenic mice induces liver neoplasia and abnormal development of the mammary gland and pancreas. Cell, 61: 1137-1146, 1990.
30. Sandgren, E. P., Luetteke, N. C, Palmiter, R. D., Brinster, R. L., and Lee, D. C. Overexpression of TGFα in transgenic mice: induction of epithelial hyperplasia, pancreatic metaplasia, and carcinoma of the breast. Cell, 61: 1121, 1990.
31. Murakami, H., Sanderson, N. D., Nagy, P., Marino, P. A., Merlino, G., and Thorgiersson, S. S. Transgenic mouse model for synergistic effects of nuclear oncogenes and growth factors in tumorigenesis: interaction of c-myc and transforming growth factor α in hepatic oncogenesis. Cancer Res., 53: 1719-1723, 1993.
32. Sandgren, E. P., Luetteke, N. C., Qiu, T. H., Palmiter, R. D., Brinster, R. L., and Lee, D. C. Transforming growth factor α dramatically enhances oncogene-induced carcinogenesis in transgenic mouse pancreas and liver. Mol. Cell. Biol., 13: 320-330, 1993.
33. Ziober, B. L., Willson, J. K. V., Hymphrey, L. E., Childress-Fields, K., and Brattain, M. G. Autocrine transforming growth factor α is associated with progression of transformed properties in human colon cancer cells. J. Biol. Chem., 268: 691-698, 1993.
34. Stoscheck, C. M., and King, L. E., Jr. Role of epidermal growth factor in carcinogenesis. Cancer Res., 46: 1030-1037, 1986.
35. Glick, A. B., Sporn, M. B., and Yuspa, S. H. Altered regulation of TGFβ1 and TGFα in primary keratinocytes and papillomas expressing v-Ha-ras. Mol. Carcinog., 4: 210-219, 1991.
36. Dlugosz, A. A., Cheng, C., Williams, E. K., Darwiche, N., Dempsey, P. J., Mann, B., Dunn, A. R., Coffey, R. J., Jr., and Yuspa, S. H. Autocrine transforming growth factor α is dispensable for v-rasHa-induced epidermal neoplasia: potential involvement of alternate epidermal growth factor receptor ligands. Cancer Res., 55: 1883-1893, 1995.
37. Lippman, S. M., Lee, J. S., Lotan, R., Hittelman, W., Wargovich, M. J., and Hong, W. K. Biomarkers as intermediate end points in chemoprevention trials. J. Natl. Cancer Inst., 82: 555-560, 1990.
38. Grandis, J. R., and Tweardy, D. J. TGFα and EGFR in head and neck cancer. J. Cell. Biochem., 17F: 188-191, 1993.
39. Bergler, W., Bier, H., and Ganzer, U. The expression of epidermal growth factor receptors in the oral mucosa of patients with oral cancer. Acta Oto-Rhino-Laryngol. Belg., 246: 121-125, 1989.
40. Shirasuna, K., Hayashido, Y., Sugiyama, M., Yoshioka, H., and Matsuya, T. Immunohistochemical localization of epidermal growth factor (EGF) and EGF receptor in human oral mucosa and its malignancy. Virchows Arch. A Pathol. Anat. Histopathol., 418: 349-353, 1991.
41. Hong, W. K., Lippman, S. M., and Wolf, G. T. Recent advances in head and neck cancer - larynx preservation and cancer chemoprevention: the Seventeenth Annual Richard and Hinda Rosenthal Foundation Award Lecture. Cancer Res., 53: 5113-5120, 1993.
42. Lippman, S. M., Garewal, H. S., and Meyskens, F. L. Retinoids as potential chemopreventive agents in squamous cell carcinoma of the head and neck. Prev. Med., 18: 740-748, 1989.
43. Beenken, S. W., Huang, P., Sellers, M., Peters, G., Listinsky, C., Stockard, C., Hubbard, W., Wheeler, R., and Grizzle, W. Retinoid modulation of biomarkers in oral leukoplakia/dysplasia. J. Cell. Biochem., 19 (Suppl.): 270-277, 1994.
44. Yoneda, K. Distribution of proliferating-cell nuclear antigen and epidermal growth factor receptor in intraepithelial squamous cell lesion of human bronchus. Mod. Pathol., 7: 480-486, 1994.
45. Rusch, V., Klimstra, D., Linkov, I., and Dmitrovsky, E. Aberrant expression of p53 or the epidermal growth factor receptor is frequent in early bronchial neoplasia, and coexpression precedes squamous cell carcinoma development. Cancer Res., 55: 1365-1372, 1995.
46. Jankowski, J., Hopwood, D., and Wormsley, K. G. Flow-cytometric analysis of growth-regulatory peptides and their receptors in Barrett's oesophagus and oesophageal adenocarcinoma. Scand. J. Gastroenterol., 27: 147-154, 1992.
47. Jankowski, J., McMenemin, R., Yu, C., Hopwood, D., and Wormsley, K. G. Proliferating cell nuclear antigen in oesophageal diseases. Correlation with transforming growth factor α expression. Gut, 33: 587-591, 1992.
48. Stemmermann, G., Heffelfinger, S. C., Noffsinger, A., Hui, Y. Z., Miller, M. A., and Fenoglio-Preiser, C. M. The molecular biology of esophageal and gastric cancer and their precursors: oncogenes, tumor suppressor genes, and growth factors. Hum. Pathol., 25: 968-981, 1994.
49. Messing, E. M., and Reznikoff, C. A. Epidermal growth factor and its receptor: marker of - and targets for - chemoprevention of bladder cancer. J. Cell. Biochem., 161: 56-62, 1992.
50. Rao, J. Y., Hemstreet, G. P., III, Hurst, R. E., Bonner, R. B., Jones, P. L., Min, K. W., and Fradet, Y. Alterations in phenotypic biochemical markers in bladder epithelium during tumorigenesis. Proc. Natl. Acad. Sci. USA, 90: 8287-8291, 1993.
51. Neal. D. R, Sharples, L., Smith, K., Fennelly, J., Hall, R. R., and Harris, A. L. The epidermal growth factor receptor and the prognosis of bladder cancer. Cancer (Phila.), 65: 1619-1625, 1990.
52. Ware, J. L. Prostate cancer progression. Implications of histopathology. Am. J. Pathol., 145: 983-993, 1994.
53. Turkeri, L. N., Sakr, W. A., Wykes, S. M.. Grignon, D. J., Pontes, J. E., and Macoska, J. A. Comparative analysis of epidermal growth factor receptor gene expression and protein product in benign, premalignant, and malignant prostate tissue. Prostate, 25: 199-205, 1994.
54. Myers, R. B., Kudlow, J. E., and Grizzle, W. E. Expression of transforming growth factor-α, epidermal growth factor and the epidermal growth factor receptor in adenocarcinoma of the prostate and benign prostatic hyperplasia. Mod. Pathol., 6: 733-737, 1993.
55. Koenders, P. G., Peters, W. H. M., Wobbes, T., Beex, L. V. A. M., Nagengast, F. M., and Bendrad, T. J. Epidermal growth factor receptor levels are lower in carcinomatous than in normal colorectal tissue. Br. J. Cancer, 65: 189-192, 1992.
56. Liu, C., Woo, A., and Tsao, M-S. Expression of transforming growth factor-α in primary human colon and lung carcinomas. Br. J. Cancer, 6: 425-429, 1990.
57. Tanaka, S., Imanishi, K., Haruma, K., Tsuda, T., Yoshihara, M., Sumii, K., and Kajiyama, G. Immunoreactive transforming growth factor-α and epidermal growth factor in colorectal adenomas and carcinomas. Oncology (Basel), 49: 381-385, 1992.
58. Markowitz, S. D., Molkentin, K., Gerbic, C., Jackson, J., Stellato, T., and Wilson, J. K. V. Growth stimulation by coexpression of transforming growth factor-α and epidermal growth factor-receptor in normal and adenomatous human colon epithelium. J. Clin. Invest., 86: 356-362, 1990.
59. Anderson, B. D., Karnes, W. E., and Pearson, R. K. Bile acids regulate the growth rate of transformed colonie epithelium and increase TGFα mRNA levels in vitro (Abstract). Gastroenterology, 104: A384, 1993.
60. Saeki, T., Stromberg, K., Qi, C-F., Gullick, W. J., Tahara, E., Normanno, N., Ciardiello, F., Kenney, N., Johnson, G. R., and Salomon, D. S. Differential immunohistochemical detection of amphiregulin and cripto in human normal colon and colorectal tumors. Cancer Res., 52: 3467-3473, 1992.
61. Goppinger, A., Wittmaack, F. M., Wintzer, H. O., Ikenberg, H., and Bauknecht, T. Localization of human epidermal growth factor receptor in cervical intraepithelial neoplasias. J. Cancer Res. Clin. Oncol., 115: 259-263, 1989.
62. Mittal, K., Pearson, J., and Demopoulos, R. Patterns of mRNA for epidermal growth factor receptor and keratin B-2 in normal cervical epithelium and in cervical intraepithelial neoplasia. Gynecol. Oncol., 38: 224-229, 1990.
63. Chapman, W. B., Lorincz, A. T., Willett, G. D., Wright, V. C., and Kurman, R. J. Epidermal growth factor receptor expression and the presence of human papilloma virus in cervical squamous intraepithelial lesions. Int. J. Gynecol. Pathol., 11: 221-226, 1992.
64. Tervahauta, A., Syrjanen, S., and Syrjanen, K. Epidermal growth factor receptor, c-erbB-2 proto-oncogene and estrogen receptor expression in human papillomavirus lesions of the uterine cervix. Int. J. Gynecol. Pathol., 13: 234-240, 1994.
65. Mitchell, M. F., Hittelman, W. N., Lotan, R., Nishioka, K., Tortolero-Luna, G., Richards-Kortum, R., and Hong, W. K. Chemoprevention trials in the cervix: design, feasibility, and recruitment. J. Cell. Biochem., 23: 104-112, 1995.
66. McGlennen, R. C., Ostrow, R. S., Carson, L. F., Stanley, M. S., and Faras, A. J. Expression of cytokine receptors and markers of differentiation in human papillomavirus-infected cervical tissues. Am. J. Obstet. Gynecol., 165: 696-705, 1991.
67. Sizemore, N., and Rorke, E. A. Human papillomavirus 16 immortalization of normal ectocervical epithelial cells alters retinoic acid regulation of cell growth and epidermal growth factor receptor expression. Cancer Res., 53: 4511-4517, 1993.
68. Meyskens, F. L., Jr., Surwit, E., Moon, T. E., Childers, J. M., Davis, J. R., Dorr, R. T., Johnson, C. S., and Alberts, D. S. Enhancement of regression of cervical intraepithelial neoplasia II (moderated dysplasia) with topically applied all-trans-retinoic acid: a randomized trial. J. Natl. Cancer Inst., 86: 539-543, 1994.
69. Klijn, J. G. M., Berns, P. M. J. J., Schmitz, P. I. M., and Foekens, J. A. The clinical significance of epidermal growth factor receptor (EGF-R) in human breast cancer: a review on 5232 patients. Endocr. Rev., 13: 3-17, 1992.
70. Ethier, S. P. Growth factor synthesis and human breast cancer progression. J. Natl. Cancer Inst., 87: 964-973, 1995.
71. van Agthoven, T., Timmermans, M., Foekens, J. A., Dorssers, L. C. J., and Henzen-Logmans, S. C. Differential expression of estrogen, progesterone, and epidermal growth factor receptors in normal, benign, and malignant human breast tissues using dual staining immunohistochemistry. Am. J. Pathol., 144: 1238-1246, 1994.
72. Fabian, C. J., Zalles, C, Kamel, S., Kimler, B. F., McKittrick, R., Tranin, A. S., Zeiger, S., Moore, W. P., Hassanein, R. S., Simon, C., Johnson, N., Vergara, G., Jewell, W. R., Lin, F., Bhatia, P., and Chin, T. Prevalence of aneuploidy, overexpressed ER, and overexpressed EGFR in random breast aspirates of women at high and low risk for breast cancer. Breast Cancer Res. Treat., 30: 263-274, 1994.
73. Gudas, L. J., Sporn, M. B., and Roberts, A. B. Cellular biology and biochemistry of the retinoids. In: M. B. Sporn, A. B. Roberts, and D. S. Goodman (eds.), The Retinoids: Biology, Chemistry, and Medicine, Ed. 2, Chap. 11, pp. 443-520. New York: Raven Press, Ltd., 1994.
74. Masui, H., Kawamoto, T., Sato, J. D., Wolf, B., Sato, G., and Mendelsohn, J. Growth inhibition of human tumor cells in athymic mice by anti-epidermal growth factor receptor monoclonal antibodies. Cancer Res., 44: 1002-1007, 1984.
75. Stavric, B. Quercetin in our diet: from potent mutagen to probable anticarcinogen. Clin. Biochem., 27: 245-248, 1994.
76. Levitzki, A. Tyrphostins: tyrosine kinase blockers as novel antiproliferative agents and dissectors of signal transduction. FASEB J., 6: 3275-3282, 1992.
77. Boulin, J. A. Tyrosine protein kinase inhibition and cancer. Int. J. Biochem., 26: 1203-1226, 1994.
78. Barnes, S., and Peterson, T. G. Biochemical targets of the isoflavone genistein in tumor cell lines. Proc. Soc. Exp. Biol. Med., 208: 103-108, 1995.
79. Barret, J. M., Ernould, A. P., Ferry, G., Genton, A., and Boutin, J. A. Integrated system for the screening of the specificity of protein kinase inhibitors. Biochem. Pharmacol., 46: 439-448, 1993.
80. Osherov, N., Gazit, A., Gilon, C., and Levitzki, A. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J. Biol. Chem., 268: 11134-11142, 1993.
81. Moon, R. C., Mehta, R. G., and Rao, K. V. N. Retinoids and cancer in experimental animals. In: M. B. Sporn, A. B. Roberts, and D. S. Goodman (eds.), The Retinoids: Biology, Chemistry, and Medicine, Ed. 2, Chap. 14, pp. 573-595. New York: Raven Press, Ltd., 1994.
82. Gazit, A., Osherov, N., Posner, I., Bar-Sinai, A., Gilon, C., and Levitzki, A. Tyrphostins. 3. Structure-activity relationship studies of α-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J. Med. Chem., 36: 3556-3564, 1993.
83. Ben-Bassat, H., Vardi, D. V., Gazit, A., Klaus, S. N., Chaouat, M., Hartzstark, Z., and Levitzki, A. Tyrphostins suppress the growth of psoriatic keratinocytes. Exp. Dermatol., 4: 82-88, 1995.
84. Yoneda, T., Lyall, R. M., Alsina, M. M., Persons, P. E., Spada, A. P., Levitzki, A., Zilberstein, A., and Mundy, G. R. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res., 51: 4430-4435, 1991.
85. Khetarpal, V. K., Markham, P. M., and Ziemniak, J. A. Dispositional characteristics of a tyrosine kinase inhibitor (RG 14620) in rats and rabbits following intravenous administration of dermal application. Drug Metab. Dispos., 22: 216-223, 1994.
86. Reddy, K. B., Mangold, G. L., Tandon, A. K., Yoneda, T., Mundy, G. R., Zilberstein, A., and Osborne, C. K. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res., 52: 3636-3641, 1992.
87. Buchdunger, E., Trinks, U., Mett, H., Regenass, U., Muller, M., Meyer, T., McGlynn, E., Pinna, L. A., Traxler, P., and Lydon, N. B. 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, 91: 2334-2338, 1994.
88. Buchdunger, E., Mett, H., Trinks, U., Regenass, U., Muller, M., Meyer, T., Beilstein, P., Wirz, B., Schneider, P., Traxler, P., and Lydon, N. B. 4,5-bis(Fluoroanilino)phthalimide: a selective inhibitor of the epidermal growth factor receptor signal transduction pathway with potent in vivo antitumor activity. Clin. Cancer Res., 1: 813-821, 1995.
89. Fry, D. W., Kraker, A. J., McMichael, A., Ambroso, L. A., Nelson, J. M., Leopold, W. R., Connors, R. W., and Bridges, A. J. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science (Washington DC), 265: 1093-1095, 1994.
90. Hook, K. E., Kunkel, M. W., Elliot, W. L., Howard, C. T., and Leopold, W. R. Epidermal growth factor receptor tyrosine kinase in A431 xenografts: inhibition by PD 153035 [4-(3-bromoanilino)-6,7-dimethoxyquinazoline]. Proc. Am. Assoc. Cancer Res., 36: 434, 1995.
91. Rewcastle, G. W., Denny, W. A., Bridges, A. J., Zhou, H., Cody, D. R., McMichael, A., and Fry, D. W. Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5′-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor. J. Med. Chem., 38: 3482-3487, 1995.
92. Ward, W. H. J., Cook, P. N., Slater, A. M., Davies, D. H., Holdgate, G. A., and Green, L. R. Epidermal growth factor receptor tyrosine kinase. Investigation of catalytic mechanism, structure-based searching and discovery of a potent inhibitor. Biochem. Pharmacol., 48: 659-666, 1994.
93. Barker, A. J., Davies, D. H. (inventors), and Imperial Chemical Industries. PLC (assignee). Pharmaceutical composition comprising quinazoline derivatives inhibit receptor tyrosine kinase(s) and are used for treating cancers e.g., leukemia(s) and tumors of breast, lung, colon, and rectum. European Patent 520,722, December 30, 1992.
94. Thompson, A. M., Bridges, A. J., Fry, D. W., Kraker, A. J., and Denny, W. A. Tyrosine kinase inhibitors. 7. 7-Amino-4-(phenylamino)- and 7-amino-4-[(phenylmethyl)amino]pyrido[4,3-d]pyrimidines: a new class of inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. J. Med. Chem., 38: 3780-3786, 1995.
95. Traxler, P., Trinks, U., Buchdunger, E., Mett, H., Meyer, T., Muller, M, Regenass, U., Rosel, J., and Lydon, N. [(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase. J. Med. Chem., 38: 2441-2448, 1995.
96. Tanaka, S., Okabe, T., Chieda, S., Endo, K., Kanoh, T., Okura, A., and Yoshida, E. BE-23372M, a novel and specific inhibitor, for epidermal growth factor receptor kinase. Jpn. J. Cancer Res., 55: 253-259, 1994.
97. Chen, H., Boiziau, J., Parker, F., Mailliet, P., Commercon, A., Tocque, B., Le Pecq, J-B., Roques, B-P., and Garbay, C. Structure-activity relationships in a series of 5-[(2,5-dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional hydrophobic aromatic interactions. J. Med. Chem., 37: 845-859, 1994.
98. Fry, D. W., Kraker, A. J., Connors, R. C., Elliott, W. L., Nelson, J. M., Showalter, H. D. H., and Leopold, W. R. Strategies for the discovery of novel tyrosine kinase inhibitors with anticancer activity. Anti-Cancer Drug Des., 9: 331-351, 1994.
99. Thompson, A. M., Rewcastle, G. W., Tercel, M., Dobrusin, E. M., Fry, D. W., Kraker, A. J., and Denny, W. A. Tyrosine kinase inhibitors. I. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2′-dithiobis(1H-indole-3-alkanoic acids). J. Med. Chem., 36: 2459-2469, 1993.
100. Palmer, B. D., Rewcastle, G. W., Thompson, A. M., Boyd, M., Showalter, H. D. H., Sercel, A. D., Fry, D. W., Kraker, A. J., and Denny, W. A. Tyrosine kinase inhibitors. 4. Structure-activity relationships among N- and 3-substituted 2,2′-dithiobis(1H-indoles) for in vitro inhibition of receptor and nonreceptor protein tyrosine kinases. J. Med. Chem., 38: 58-67, 1995.
101. Cushman, M., Zhu, H., Geahlen, R. L., and Kraker, A. J. Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src. J. Med. Chem., 37: 3353-3362, 1994.
102. Andrews, D. M., Gregoriou, M, Page, T. C. M., Peach, J. M., and Pratt, A. J. Potential mechanism-based tyrosine kinase inhibitors. Part 2. Design and synthesis of peptides containing heterocyclic tyrosine analogues. J. Chem. Soc. Perkin Trans. I, 11: 1335-1340, 1995.
103. Gimenez-Conti, I. B., and Slaga, T. J. The hamster cheek pouch carcinogenesis model. J. Cell. Biochem., 17F: 83-90, 1993.
104. Shin, D. M., Gimenez, I. B., Lee, J. S., Nishioka, K., Wargovich, M. J., Thacher, S., Lotan, R., Slaga, T. J., and Hong, W. K. Expression of epidermal growth factor receptor, polyamine levels, ornithine decarboxyase activity, micronuclei, and transglutaminase I in a 7,12-dimethylbenz(a)anthracene-induced hamster buccal pouch carcinogenesis model. Cancer Res., 50: 2505-2510, 1990.
105. Steele, V. E., Moon, R. C., Lubet, R. A., Grubbs, C. J., Reddy, B. S., Wargovich, M., McCormick, D. L., Pereira, M. A., Crowell, J. A., Bagheri, D., Sigman, C. C., Boone, C. W., and Kelloff, G. J. Preclinical efficacy evaluation of potential chemopreventive agents in animal carcinogenesis models: methods and results from the NCI chemoprevention testing program. J. Cell. Biochem. Suppl., 20: 32-54, 1994.
106. Burke, T. R., Jr. Protein-tyrosine kinases: potential targets for anticancer drug development. Stem Cells, 12: 1-6, 1994.
107. Hubbard, S. R., Wei, L., Ellis, L., and Hendrickson, W. A. Crystal structure of the tyrosine kinase domain of the human insulin receptor. Nature (Lond.), 372: 746-754, 1994.
108. Knighton, D. R., Cadena, D. L., Zheng, J., Ten Eyck, L. F., Taylor, S. S., Sowadski, J. M., and Gill, G. N. Structural features that specify tyrosine kinase activity deduced from homology modeling of the epidermal growth factor receptor. Proc. Natl. Acad. Sci. USA, 90: 5001-5005, 1993.