Specific inhibition of epidermal growth factor receptor tyrosine kinase by 4-anilinoquinazolines

Breast Cancer Research and Treatment

Volumn 38, Issue 1, 1996, Pages 67-73

  Wakeling, A E ^a   Barker, A J ^a   Davies, D H ^a   Brown, D S ^a   Green, L R ^a   Cartlidge, S A ^a   Woodburn, J R ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

EGF receptor; Epidermal growth factor; IGF I; Quinazolines; TGF ; Tyrosine kinase inhibitor

Indexed keywords

4 (3 CHLOROANILINO)QUINAZOLINE; 4 ANILINOQUINAZOLINE; ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR; EPIDERMAL GROWTH FACTOR RECEPTOR; PROTEIN TYROSINE KINASE; QUINAZOLINE DERIVATIVE; SOMATOMEDIN C; TRANSFORMING GROWTH FACTOR ALPHA; UNCLASSIFIED DRUG;

AUTOPHOSPHORYLATION; BREAST CANCER; CANCER CELL CULTURE; CELL GROWTH; CELL STIMULATION; CHEMICAL STRUCTURE; CONCENTRATION RESPONSE; CONFERENCE PAPER; CONTROLLED STUDY; ENZYME INHIBITION; GROWTH INHIBITION; HUMAN; HUMAN CELL; MITOGENESIS; PRIORITY JOURNAL; SQUAMOUS CELL CARCINOMA;

ANTINEOPLASTIC AGENTS; ENZYME INHIBITORS; HUMANS; KB CELLS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED;

EID: 0030061424     PISSN: 01676806     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF01803785     Document Type: Conference Paper

References (25)

1. Sainsbury JRC, Malcolm AJ, Appleton DR, Farndon JR, Harris AL: Presence of epidermal growth factor receptor as an indicator of poor prognosis in patients with breast cancer. J Clin Pathol 38:1225-1228, 1985.
2. Gullick WJ: Prevalence of aberrant expression of the epidermal growth factor receptor in human cancers. Br Med Bull 47:87-98, 1991.
3. Rajkumar T, Gullick WJ: The Type I growth factor receptors in human breast cancer. Breast Cancer Res Treat 29:3-9, 1994.
4. Yarden Y, Ullrich A: Growth factor receptor tyrosine kinases. Ann Rev Biochem 57:443-478, 1998.
5. Schlessinger J: How receptor tyrosine kinases activate Ras. Trends Biochem Sci 18:273-275, 1993.
6. Ennis BW, Lippman ME, Dickson RB: The EGF receptor system as a target for antitumor therapy. Cancer Investigation 9:553-562, 1991.
7. Workman P: The potential for molecular oncology to define new drug targets. In Kerr DJ, Workman P (eds) New Molecular Targets for Cancer Chemotherapy. CRC Press, London, 1994, pp 1-29.
8. Burke TR Jr: Protein-tyrosine kinase inhibitors. Drugs of the Future 17:119-131, 1992.
9. Hanks SK: Eukaryotic protein kinases. Current Opin Struct Biol 1:369-383, 1991.
10. Yaish P, Gazit A, Gilon C, Levitzki A: Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors. Science 242:933-935, 1988.
11. Ward WHJ, Cook PN, Slater AM, Davies DH, Holdgate GA, Green LR: 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.
12. Mosmann T: Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. J Immunol Methods 56:55-63, 1983.
13. Posner I, Engel M, Levitzki A: Kinetic model of the epidermal growth factor (EGF)-receptor tyrosine kinase and a possible mechanism of its activation by EGF. J Biol Chem 267:20638-20647, 1992.
14. Levitzki A: Tyrphostins - potential antiproliferative agents and novel molecular tools. Biochem Pharmacol 40:913-918, 1990.
15. Thompson AM, Rewcastle GW, Tercel M, Dobrusin EM, Fry DW, Kraker AJ, Denny WA: Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,4-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2′-dithiobis(1H-indole-3-alkanoic acids). J Med Chem 36:2459-2469, 1993.
16. Buchdunger E, Trinks U, Mett H, Regenass U, Muller M, Meyer T, McGlynn E, Pinna LA, Traxler P, Lydon NB: 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.
17. Fry DW, Kraker AJ, McMichael A, Ambroso LA, Nelson JM, Leopold WR, Connors RW, Bridges AJ: A specific inhibitor of epidermal growth factor receptor tyrosine kinase. Science 265:1093-1095, 1994.
18. Osherov N, Gazit A, Gilon C, Levitzki A: Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins. J Biol Chem 268: 11134-11142, 1993.
19. Vignon F, Bouton M-M, Rochefort H: Antiestrogens inhibit the mitogenic effect of growth factors on breast cancer cells in the total absence of estrogens. Biochem Biophys Res Commun 146:1502-1508, 1987.
20. Koga M, Sutherland RL: Epidermal growth factor partially reverses the inhibitory effects of antioestrogens on T47D human breast cancer cell growth. Biochem Biophys Res Commun 146:739-747, 1987.
21. Wakeling AE, Newboult E, Peters SW: Effects of antioestrogens on the proliferation of MCF-7 human breast cancer cells. J Molec Endocr 2:225-234, 1989.
22. Ignar-Trowbridge DM, Nelson KG, Bidwell MC, Curtis SW, Washburn TF, McLachlan JA, Korach KS: Coupling of dual signalling pathways: Epidermal growth factor action involves the estrogen receptor. Proc Natl Acad Sci USA 89:4658-4662, 1992.
23. Newton CJ, Buric R, Trapp T, Brockmeier S, Pagotto U, Stalla GK: The unliganded estrogen receptor (ER) transduces growth factor signals. J Steroid Biochem Mol Biol 48:481-486, 1994.
24. Reddy KB, Mangold GL, Tandon AK, Yoneda T, Mundy GR, Zilberstein A, Osborne CK: Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res 52:3636-3641, 1992.
25. Yoneda T, Lyall RM, Alsina MM, Persons PE, Spada AP, Levitzki A, Zilberstein A, Mundy GR: 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.