Inhibition of transforming activity of the ret/ptc1 oncoprotein by a 2- indolinone derivative

International Journal of Cancer

Volumn 85, Issue 3, 2000, Pages 384-390

  Lanzi, Cinzia ^a   Cassinelli, Giuliana ^a   Pensa, Tiziana ^a   Cassinis, Marco ^a   Gambetta, Romolo A ^a   Borrello, Maria G ^a   Menta, Ernesto ^b   Pierotti, Marco A ^a   Zunino, Franco ^a  

^a NATIONAL CANCER INSTITUTE   (Italy)

^b Novuspharma SpA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

INDOLE DERIVATIVE; ONCOPROTEIN; PROTEIN TYROSINE KINASE;

ANIMAL CELL; ARTICLE; CELL PROLIFERATION; ENZYME ACTIVITY; ENZYME INHIBITION; GENE EXPRESSION; MALIGNANT TRANSFORMATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION;

ANIMALS; BLOTTING, WESTERN; CARCINOMA, SQUAMOUS CELL; ENZYME INHIBITORS; GENES, RAS; HUMANS; INDOLES; KINETICS; MICE; ONCOGENE PROTEINS, FUSION; PHENOTYPE; PRECIPITIN TESTS; PROTEIN-TYROSINE KINASES; SIGNAL TRANSDUCTION; THYROID NEOPLASMS; TUMOR CELLS, CULTURED; URINARY BLADDER NEOPLASMS;

EID: 0033989107     PISSN: 00207136     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1097-0215(20000201)85:3<384::AID-IJC15>3.0.CO;2-Y     Document Type: Article

References (22)

1. BORRELLO, M.G., ALBERTI, L., ARIGHI, E., BONGARZONE, I., BATTISTINI, C., BARDELLI, A., PASINI, B., PIUTTI, C., RIZZETTI, M.G., MONDELLINI, P., RADICE, M.T. and PIEROTTI, M.A., The full oncogenic activity of ret/ptc2 depends on tyrosine 539, a docking site for phospholipase Cγ. Mol. cell. Biol., 16, 2151-2163 (1996).
2. BORRELLO, M.G., PELICCI, G.A., ARIGHI, E., DE FILIPPIS, L., GRECO, A., BONGARZONE, I., RIZZETTI, M.G., PELICCI, P.G. and PIEROTTI, M.A., The oncogenic version of the ret and trk tyrosine kinases bind shc and grb2 adaptor proteins. Oncogene, 9, 1661-1668 (1994).
3. BUZZETTI, F., BRASCA, M.G., CRUGNOLA, A., FUSTINONI, S., LONGO, A. and PENCO, S., Cinnamamide analogs as inhibitors of protein tyrosine kinases. Il Farmaco. 48, 615-636 (1993).
4. DURICK, K., YAO, V.J., BORRELLO, M.G., BONGARZONE, I., PIEROTTI, M.A. and TAYLOR, S.S., Mitogenic activity of ret/ptc2 is due to dimerization via the type-1 regulatory sub-unit of protein kinase A. J. biol. Chem., 270, 24642-24645 (1995).
5. FONG, T.A., SHAWVER, L.K., SUN, L., TANG, C., APP, H., POWELL, T.J., KIM, Y.H., SCHRECK, R., WANG, X., RISAU, W., HIRTH, K.P. and MCMAHON, G., SU5416 is a potent and selective inhibitor of the vascular endothelial-growth-factor receptor (Flk-1/KDR) that inhibits tyrosine-kinase catalysis, tumor vascularization and growth of multiple tumor types. Cancer Res., 59, 99-106 (1999).
6. GAZIT, A., YAISH, P., GILON, C. and LEVITZKI, A., Tyrphostins I: synthesis and biological activity of protein tyrosine-kinase inhibitors. J. med. Chem., 32, 2344-2352 (1989).
7. GEISSLER, J.F., TRAXLER, P., REGENASS, U., MURRAY, B.J., ROESEL, J.L., MEYER, T., MCGLYNN, E., STORNI, A. and LYDON, N.B., Thiazolidinediones. Biochemical and biological activity of a novel class of tyrosine protein-kinase inhibitors. J. biol. Chem., 265, 22255-22261 (1990).
8. GRIECO, M., SANTORO, M., BERLINGIERI, M.T., MELILLO, R.M., DONGHI, R., BONGARZONE, I., PIEROTTI, M.A., DELLA PORTA, G., FUSCO, A. and VECCHIO, G., PTC is a novel rearranged form of the ret proto-oncogene and is frequently detected in vivo in human thyroid papillary carcinomas. Cell, 60, 557-563 (1990).
9. KLOHS, W.D., FRY, D.W. and KRAKER, A.J., Inhibitors of tyrosine kinase. Curr. Opin. Oncol., 9, 562-568 (1997).
10. LANZI, C., BORRELLO, M.G., BONGARZONE, I., MIGLIAZZA, A., FUSCO, A., GRIECO, A., SANTORO, A., GAMBETTA, R.A., ZUNINO, F., DELLA PORTA, G. and PIEROTTI, M.A., Identification of the product of two oncogenic rearranged forms of the ret proto-oncogene in papillary thyroid carcinomas. Oncogene, 7, 2189-2194 (1992).
11. LANZI, C., PENSA, T., CASSINIS, M., CORTI, C., GAMBETTA, R.A., PRATESI, G., MENTA, E., ARDINI, E. and ZUNINO, F., A cell- and mechanism-based approach for the selection of EGF receptor inhibitors. Anti-Cancer Drug Des., 12, 515-524 (1997).
12. LE COUTRE, P., MOLOGNI, L., CLERIS, L., MARCHESI, E., BUCHDUNGER, E., GIARDINI, R., FORMELLI, F. and GAMBACORTI-PASSERINI, C., In vivo eradication of human BCR/ABL-positive leukemic cells with an ABL kinase inhibitor. J. nat. Cancer Inst., 91, 163-168 (1999).
13. LEVITZKI, A., Tyrphostins: tyrosine-kinase blockers as novel anti-proliferative agents and dissectors of signal transduction. FASEB J., 6, 3275-3282 (1992).
14. LEVITZKI, A. and GAZIT, A., Tyrosine kinase inhibition: an approach to drug development. Science, 267, 1782-1788 (1995).
15. LEVITZKI, A., GAZIT, A., OSHEROV, N., POSNER, I. and GILON, C., Inhibition of protein-tyrosine kinases by tyrphostins. Methods Enzymol., 201, 347-361 (1991).
16. LOWENSTEIN, E.J., DALY, R.J., BATZER, A.G., LI, W., MARGOLIS, B., LAMMERS, R., ULLRICH, A., SKOLNIK, E.Y., BAR-SAGI, D. and SCHLESSINGER, J., The SH2- and SH3-domain-containing protein GRB2 links receptor tyrosine kinases to ras signaling. Cell, 70, 431-442 (1992).
17. MOHAMMADI, M., MCMAHON, G., SUN, L., TANG, C., HIRTH, P., YEH, B.K., HUBBARD, S.R. and SCHLESSINGER, J., Structures of the tyrosine-kinase domain of fibroblast-growth-factor receptor in complex with inhibitors. Science, 276, 955-969 (1997).
18. PASINI, B., CECCHERINI, I. and ROMEO, G., ret mutations in human disease. Trends Genet., 12, 138-144 (1996).
19. PIEROTTI, M.A. and 12 OTHERS, Characterization of an inversion of the long arm of chromosome 10 juxaposing D10S170 and ret and creating the oncogene sequence ret/ptc. Proc. nat. Acad. Sci. (Wash.), 89, 1616-1620 (1992).
20. 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).
21. TANIGUCHI, M., UEHARA, Y., MATSUYAMA, M. and TAKAHASHI, M., Inhibition of ret tyrosine-kinase activity by herbimycin A. Biochem. biophys. Res. Commun., 195, 208-214 (1993).
22. YONEDA, T., LYALL, R.M., ALSINA, M.M., PERSON, P.E., SPADA, A.P., LEVITZKI, A., ZILBERSTEIN, A. and MUNDY, G.R., The anti-proliferative effects of tyrosine-kinase inhibitors tyrphostins on a human squamous-cell carcinoma in vitro and in nude mice. Cancer Res., 51, 4430-4435 (1991).