Characterization of the effects of the novel non-steroidal antiestrogen EM-800 on basal and estrogen-induced proliferation of T-47D, ZR-75-1 and MCF- 7 human breast cancer cells in vitro

International Journal of Cancer

Volumn 73, Issue 1, 1997, Pages 104-112

  Simard, Jacques ^a   Labrie, Claude ^a   Bélanger, Alain ^a   Gauthier, Sylvain ^a   Singh, Shankar M ^a   Mérand, Yves ^a   Labrie, Fernand ^a  

^a LAVAL UNIVERSITY   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

4 [4 METHYL 2 [4 [2 (1 PIPERIDINYL)ETHOXY]PHENYL] 7 PIVALOYLOXY 2H 1 BENZOPYRAN 3 YLPHENYL] PIVALATE; ANTIESTROGEN; DROLOXIFENE; FULVESTRANT; N BUTYL 11 (3,17BETA DIHYDROXYESTRA 1,3,5(10) TRIEN 7ALPHA YL) N METHYLUNDECANAMIDE; TAMOXIFEN; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CELL GROWTH; CELL PROLIFERATION; HUMAN; HUMAN CELL; PRIORITY JOURNAL;

BENZOPYRANS; BREAST NEOPLASMS; CELL DIVISION; ESTRADIOL; ESTROGEN ANTAGONISTS; FEMALE; HUMANS; PROPIONATES; TAMOXIFEN; TUMOR CELLS, CULTURED;

EID: 0030879732     PISSN: 00207136     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1097-0215(19970926)73:1<104::AID-IJC16>3.0.CO;2-G     Document Type: Article

References (35)

1. BUNONE, G., BRIAND, P.-A., MIKSICEK, R.J. and PICARD, D., Activation of the unliganded estrogen receptor by EGF involves the MAP kinase pathway and direct phosphorylation. EMBO J., 15, 2174-2183 (1996).
2. CANNEY, P.A., GRIFFITHS, T., LATIEF, T.N. and PRIESTMAN, T.J., Clinical significance of Tamoxifen withdrawal response. Lancet, 1, 36 (1987).
3. CHALBOS, D., PHILIPS, A., GALTIER, F. and ROCHEFORT, H., Synthetic antiestrogens modulate induction of pS2 and cathepsin-D messenger ribonucleic acid by growth factors and adenosine 3′,5′-monophosphate in MCF7 cells. Endocrinology, 133, 571-576 (1993).
4. 50) on an enzymatic reaction. Biochem. Pharmcol., 22, 3099-3108 (1973).
5. CHETRITE, G. and PASQUALINI, J.G., Biological responses of ICI 164, 384 and other antiestrogens in vaginal and uterine cells of fetal guinea pig in culture. Acta Endocrinol 125, 401-408 (1991).
6. COUILLARD, S., LABRIE, C., GAUTHIER, S., MÉ RAND, Y. and LABRIE, F., Highly potent and pure antiestrogenic activity of a new antiestrogen on human ZR-75-1 breast tumors in nude mice. Proc. Endocrine Society Meeting Vol. 1, p. 604. San Francisco (1996).
7. DEFRIEND, D.J., ANDERSON, E., BELL, J., WILKS, D.P., WEST, C.M., MANSEL, R.E. and HOWELL, A., Effects of 4-hydroxyiamoxifen and a novel pure antioestrogen (ICI 182780) on the clonogenic growth of human breast cancer cells in vitro. Brit. J. Cancer. 70, 204-211 (1994).
8. GALLO, M.A. and KAUFMAN, D., Antagonistic and agonistic effects of Tamoxiten: significance in human cancer. Semin. Oncol., 24 (Suppl. 1):S1-71-S1-80 (1997).
9. GALTHIER, S. and 15 OTHERS. (S)-(+)-[7-(2.2-dimethyl-I-oxopropoxy)-4-methyl-2-[4-12-(1piperidinyl)ethoxy] phenyl]-2H-1benzopyran-3-yl]phenyl]-2.2-dimeihylpropanoate (EM-800): a highly potent, specific and orally active non-steroidal antiestrogen. J. med. Chem. (1997) (in press).
10. GIAMBIAGI, N. and PASQUALINI, J.R., Studies on the activation of the oestrogen receptor bound to the anti-oestrogens 4-hydroxytamoxifen and ICI 164.384 by using three monoclonal antibodies. J. mol. Endocrinol., 7, 9-19 (1991).
11. GOTTARDIS, M.M. and JORDAN, V.C., Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration. Cancer Res., 48, 5183-5187 (1988).
12. HOWELL, A., DODWELL, D.J., ANDERSON, H. and REDFORD, J., Response after withdrawal of tamoxifen and progestogens in advanced breast cancer. Ann. Oncol., 3, 611-617 (1992).
13. JORDAN, V.C., Molecular mechanisms of antiestrogen action in breast cancer. Breast Cancer Res Treat., 31, 4837-1844, (1994).
14. JORDAN, V.C. and ASSIKIS, V.J., Endometrial carcinoma and Tamoxifen: clearing up a controversy. Clin Cancer Res., 1, 467-172, (1995).
15. KATO, S., ENDOH, H., MASUHIRO, Y., KITAMOTO, T., UCHIYAMA, S., SASAKI, H., MASUSHIGE, S., GOTOH, Y., NISHIDA, E., KAWASHIMA, H., METZGER, D. and CHAMBON, P., Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science, 270, 1491-1494 (1995).
16. LABRIE, C., MARTEL, C., DUFOUR, J.M., LÉVESQUE, C., MÉRAND, Y. and LABRIT, F., Novel compounds inhibit estrogen formation and action. Cancer Res., 52, 610-615 (1992).
17. LABRIE, F., Intracrinology. Mol. cell. Endocrinol., 78, C113-C118 (1991).
18. LÉVESQUE, C., MERAND, Y., DUFOUR, J.M., LABRIE, C. and LABRIE, F., Synthesis and biological activity of new halo-steroidal antiestrogens. J. med. Chem., 34, 1624-1030 (1991).
19. LIEN, E.A., SOLHEIM, E. and UELAND, P.M., Distribution of Tamoxifen and its metabolites in rat and human tissues during steady-state treatment. Cancer Res. 51, 4837-4844 (1991).
20. LÖSER, R., SEIBEL, K., ROOS, W. and EPPENBERGER, U., In vivo and in vitro antiestrogenic action of 3-hydroxytamoxifen, tamoxifen, and 4-hydroxytamoxifen. Europ. J. Cancer clin. Oncol., 21, 985-990 (1985).
21. MACMAHON, B., Overview of studies on endometrial cancer and other types of cancer in humans: perspectives of an epidemiologist, Semin. Oncol., 24 (Suppl. 1):S1-122-S1-139 (1997).
22. MARTEL, C., GAUTHIER, S., MÉRAND, Y., LI, X., PROVENCHER, L. and LABRIE, K. Comparison of the effects of the new antiestrogens EM-800 and ICI 182780 on estrogen-sensitive parameters in the overiectmozed mouse. Proc. 10th Int. Congress of Endocrinology. San Francisco. 152. Abstract P1-71. (1996).
23. ORMEROD, G.M. and KUBBIES, M., Cell cycle analysis of asynchronous cell populations by flow cytometry using bromodeoxyuridine label and Hoesehstpropidium iodide stain. Cytometry. 13, 678-685 (1992).
24. PARKER, S.L., TONG, T., BOLDES, S. and WINGO, P.A., Cancer statistics 1997. CA Cancer J. Clin., 46, 5-27 (1997).
25. POULIN, R., MÉRAND, Y., POIRIER, D., LÉVESQUE, C., DUFOUR, J.M. and LABRIE, F., Amiestrogenic properties of keoxifenc. trans-4-hydroxytamoxifen and ICI164384. a new steroidal antiestrogen, in ZR-75-1 human breast cancer cells. Breast Cancer Res. Treat,. 14, 65-76 (1989).
26. POWLES, T.J. Efficacy of tamoxifen as treatment of breast cancer. Semin. Oncol., 24, (Suppl. 1) S1-48-S1-54 (1997).
27. ROBERTSON, D.W., KATZENELLENBOGEN, J.A., LONG, D.J., RORKE, E.A. and KATZENELLENBOGEN, B.S., Tamoxifen antiestrogens. A comparison of the activity, pharmacokinetics. and metabolic activation of the cis and trans isomers of tamoxifen. J. Steroid Biochem., 16, 1-13 (1982).
28. RODBARD, D., Apparent positive cooperative effect in cyclic AMP and corticosteroid production by isolated adrenal cells in response to ACTH analogs. Endocrinology, 94, 1427-1437 (1974).
29. SIMARD, J., DAUVOIS, S., HAAGENSEN, D.E., LÉVESQUE, C., MÉRAND, Y. and LABRIE, F., Regulation of progesterone-binding breast cyst protein GC-DFP-24 secretion by estrogens and androgens in human breast cancer cells: a new marker of steroid action in breast cancer. Endocrinology. 126. 3223-3231 (1990).
30. SIMARD, J., SASCHEZ, R., POIRIER, D., GAUTHIER, S., SINGH, M.S., MÉRAND, Y. BÉLAGER, A., LABRIE, C., and LABRIE, F., Blockade of the stimulatory effect of estrogens. OH-Tamoxifen. OH-Toremifene, Droloxifene and Raloxifene on alkaline phosphatase activity by antiestrogen EM-800 in human endometrial adenocarcinoma Ishikawa cells, Cancer Res. 57, 3494-3497 (1997).
31. TREMBLAY, G.B., TREMBLAY, A., COPELAND, N.G., GILBERT, D.J., JENKINS, N.A., LABRIE, R. and GIGUÉRE, V. Cloning, chromosomal localization, and functional analysis of the murine estrogen receptor β. Mol, Endrocrinol., 11. 353-365 (1997).
32. VALAVAARA, R., Phase II trials with Toremifene in advanced breast cancer: a review. Breast Cancer Res. Treat., 16 (Suppl.). 531-535 (1990).
33. WAKELING, A.E., The future of new pure antiestrogens in clinical breast cancer. Breast Cancer Res. Treat., 25, 1-9 (1993).
34. WAKELING, A.E. and BOWLER, J., ICI 182, 780, a new antioestrogen with clinical potential. J. Steroid Biochem. mol. Biol., 43, 173-177 (1992).
35. WEAVER, C.A., SPRINGER, P.A. and KATZENELLENBOGEN, B.S., Regulation of pS2 gene expression by affinity labeling and reversibly binding estrogens and antiestrogens: comparison of effects on the native gene and on pS2-ehloramphenicol acetyltransferase fusion genes transfected into MCF-7 human breast cancer cells. Mol. Endocrinol., 2, 936-945 (1988).