Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative

Cancer Research

Volumn 56, Issue 1, 1996, Pages 100-104

  Buchdunger, Elisabeth ^a   Zimmermann, Jürg ^a   Mett, Helmut ^a   Meyer, Thomas ^a   Müller, Marcel ^a   Druker, Brian J ^b   Lydon, Nicholas B ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 ANILINOPYRIMIDINE DERIVATIVE; EPIDERMAL GROWTH FACTOR; IMATINIB; INSULIN; INTERLEUKIN 3; PLATELET DERIVED GROWTH FACTOR RECEPTOR; PROTEIN TYROSINE KINASE INHIBITOR; SOMATOMEDIN C; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; AUTOPHOSPHORYLATION; CANCER INHIBITION; CONTROLLED STUDY; DRUG MECHANISM; ENZYME INHIBITION; ENZYME REGULATION; FEMALE; INHIBITION KINETICS; INTRAPERITONEAL DRUG ADMINISTRATION; MALIGNANT TRANSFORMATION; MOUSE; NONHUMAN; ONCOGENE; PRIORITY JOURNAL;

3T3 CELLS; ANIMALS; CELL LINE, TRANSFORMED; GROWTH SUBSTANCES; MICE; MICE, INBRED BALB C; ONCOGENE PROTEINS V-ABL; PIPERAZINES; PIPERIDINES; PROTO-ONCOGENE PROTEINS C-FOS; PYRIMIDINES; RECEPTORS, PLATELET-DERIVED GROWTH FACTOR; TUMOR CELLS, CULTURED;

EID: 0030031766     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (35)

1. Abelson, H. T., and Rabstein, L. S. Lymphosarcoma: virus-induced thymic-independent disease in mice. Cancer Res., 30: 2213-2222, 1995.
2. Rosenberg, N , and Witte, O. N. Abelson murine leukemia virus mutants with alterations in the virus specific p120 molecule. J. Virol , 33. 340-348, 1980
3. Wang, J Y , Queen, C., and Baltimore, D. Expression of Abelson murine leukemia virus-encoded protein in E coli causes extensive phosphorylation of tyrosine residues J. Biol. Chem., 257: 13181-13184, 1994.
4. Baltimore, D., Rosenberg, N , and Witte, O N. Transformation of immature lymphoid cells by Abelson murine leukemia virus. Immunol. Rev. 48: 3-22, 1994
5. Rosenberg, N., Baltimore, D., and Scher, C. D. In vitro transformation of lymphoid cells by Abelson murine leukemia virus. Proc. Natl. Acad Sci. USA, 72. 1932-1936, 1975
6. Goff, S P , Gilboa, E., Witte, O. N., and Baltimore, D Structure of the Abelson murine leukemia virus genome and the homologous cellular gene, studies with cloned viral DNA. Cell, 22: 777-785, 1980.
7. Deisseroth, A. B., Andreeff, M. Champlin, R., Keating, M. J., Kantarjian, H., Khoun, I. F , and Talpaz, M. Chronic Leukemias. In: V. T. De Vita (ed.), Cancer: Principles and Practice of Oncology, pp. 1965-1979 Philadelphia. J. B Lippincott Company, 1994
8. Nowell, P. C., and Hungerford, D. A. A minute chromosome in human chronic granulocytic leukemia. Science (Washington DC), 132: 1497, 1960.
9. Groffen, J., Stephenson, J. R., Heisterkamp, N., and de Klein, A. Philadelphia chromosome breakpoints are clustered within a limited region, bcr, on chromosome 22. Cell, 36: 93-99, 1984.
10. Shtivelman, E., Lifshitz, B., Gale, R. P , and Canaani, E. Fused transcript of abl and bcr genes in chronic myelogenous leukaemia. Nature (Lond.), 315: 550-554, 1985.
11. Clark, S. S., McLaughlin, J., Timmons, M., Pendergast, A. M., Ben Neriah, Y., Dow, L. W., Crist, W., Rovera, G., Smith, S. D , and Witte, O. N. Expression of a distinctive BCR-ABL oncogene in Ph1-positive acute lymphocytic leukemia (ALL). Science (Washington DC), 239: 775-777, 1988.
12. Clark, S S., McLaughlin, J., Crist, W. M , Champlin, R., and Witte, O. N. Unique forms of the abl tyrosine kinase distinguish Ph1-positive CML from Ph1-positive ALL. Science (Washington DC), 235: 85-88, 1987.
13. Fainstein, E., Marcelle, C., Rosner, A., Canaani, E., Gale, R. P., Dreazen, O., Smith, S. D., and Croce, C. M. A new fused transcript in Philadelphia chromosome positive acute lymphocytic leukaemia. Nature (Lond.), 330: 386-388, 1987.
14. Heisterkamp, N., Stam, K., Groffen, J., de Klein, A., and Grosveld, G. Structural organization of the bcr gene and its role in the Ph′ translocation. Nature (Lond.), 315: 758-761, 1985.
15. Kurzrock, R , Gutterman, J. U., and Talpaz, M. The molecular genetics of Philadelphia chromosome-positive leukemias. N. Engl. J. Med., 319: 990-998, 1988.
16. Lugo, T. G , Pendergast, A M., Muller, A. J., and Witte, O. N Tyrosine kinase activity and transformation potency of bcr-abl oncogene products. Science (Washington DC), 247: 1079-1082, 1990
17. Konopka, J. B., Watanabe, S. M., and Witte, O. N. An alteration of the human c-Abl protein in K562 leukemia cells unmasks associated tyrosine protein kinase activity. Cell, 37: 1035-1042, 1984.
18. bcr/abl gene of the Philadelphia chromosome. Science (Washington DC), 247: 824-830, 1990.
19. Kelliher, M. A., McLaughlin, J , Witte, O. N., and Rosenberg, N. Induction of chronic myelogenous leukemia in mice by the v-abl and BCR/ABL. Proc Natl. Acad. Sci. USA, 87: 6649-6653, 1990.
20. Daley, G Q. Animal models of BCR/ABL-induced leukemias. Leuk & Lymphoma , 11 (Suppl. 1): 57-60, 1993.
21. Heisterkamp, N , Jenster, G., ten Hoeve, J., Zovich, D., Pattengale, P. K., and Groffen, J. Acute leukaemia in bcr/abl transgenic mice. Nature (Lond.), 344: 251-253, 1990
22. Geissler, J. F., Roesel, J , Meyer, T., Trinks, U. P., Traxler, P., and Lydon, N. B. Benzopyranones and benzothiopyranones: a class of tyrosine protein kinase inhibitors with selectivity for the v-abl kinase. Cancer Res., 52: 4492-4498, 1992.
23. bcr/abl tyrosine kinase activity induces K562 to differentiate. Blood, 82: 3524-3529, 1993.
24. Buchdunger, E., Zimmermann, J., Mett, H., Meyer, T., Muller, M., Regenass, U , and Lydon, N. B. Selective inhibition of the platelet-derived growth factor signal transduction pathway by a novel tyrosine protein kinase inhibitor of the 2-phenylamino pyrimidme class Proc. Natl. Acad. Sci. USA, 92: 2558-2562, 1995.
25. Ochi, S , Fujiwara, Y., Yokoyama, K., Fukunaga, M., Shin, S., Orita, Y., Fukuhara, Y , Ueda, N , and Kamada, T Signaling mechanism of platelet-derived growth factor in cultured rat mesangial cells. Contrib. Nephrol., 95. 48-53, 1991.
26. Nair, A. P., Hirsch, H. H., and Moroni, C. Mast cells sensitive to v-H-ras transformation are hyperinducible for interleukin 3 expression and have lost tumor-suppressor activity. Oncogene, 7 1963-1972, 1992.
27. Lee, J. C., Hapel, A. J., and Ihle, J. N. Constitutive production of a unique lymphokine (IL-3) by the WEHI-3 cell line. J. Immunol., 128: 2393-2398, 1982.
28. Druker, B J , Mamon, H. J., and Roberts, T. M. Oncogenes, growth factors, and signal transduction. N Engl. J. Med., 321: 1383-1391, 1989
29. Buchdunger, E , Trinks, U., Mett, H., Regenass, U., Mueller, 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 viva antitumor activity Proc. Natl Acad. Sci. USA, 91: 2334-2338, 1994.
30. Meyer, T , Regenass, U., Fabbro, D., Alten, E., Roesel, J., Mueller, M., Caravatti, G , and Matter, A. A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and in vitro proliferative as well as in vivo anti-tumor activity Int J Cancer, 43. 851-856, 1989.
31. Evans, B D., Smith, I. E., Shorthouse, A. J., and Millar, J. J. A comparison of the response of human lung cell carcinoma to vindesine and vincristine. Br. J. Cancer. 45 466-468, 1982
32. Furet, P , Caravatti, G., Lydon, N , Priestle, J. P., Sowadski, J. M., Trinks, U., and Traxler, P. Modelling study of protein kinase inhibitors: Binding mode of staurosporine-origin of the selectivity of CGP 52411. J Comput. Aided Mol. Des., in press, 1995.
33. Heisterkamp, N., Stephenson, J R., Groffen, J., Hansen, P. F., de Klein, A., Bartram, C. R., and Grosveld, G. Localization of the c-abl oncogene adjacent to a translocation point in chronic myelocytic leukemia. Nature (Lond.), 306: 239-242, 1995
34. Elefanty, A. G., Hariharan, I. K., and Cory, S bcr-abl, the hallmark of chronic myeloid leukaemia in man, induces multiple haemopoietic neoplasms in mice. EMBO J., 9: 1069-1078, 1990.
35. Heldin, C H , and Westermark, B. Platelet-derived growth factor: mechanism of action and possible in vivo function. Cell Regul., 1: 555-566, 1990