Unexpected oestrogenic activity in a derivative of antioestrogenic triphenylethylenes
Chapter
Abstract
Non-steroidal antioestrogens are a group of pharmacological agents that inhibit oestradiolstimulated events both in vivo and in vitro (Sutherland & Jordan, 1981). There is considerable evidence to suggest that the antagonism of oestradiol action is competitive via the oestrogen receptor (Jordan, 1984); however, the precise molecular mechanism of action is unknown.
Keywords
Test Compound Precise Molecular Mechanism Relative Binding Affinity Estrogen Receptor Binding Antiestrogen Action
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References
- ACTON, D., HILL, G., & TAIT, B.S. (1983). Tricyclic triarylethylene antiestrogens: dibenz (b.f.) oxepins, dibenzo (b.f.), thiepins dibenzo (a,e) cytoctenes and dibenzo (b.f.) thiocins. J. med. Chem., 26, 1131–1137.PubMedCrossRefGoogle Scholar
- BORGNA, J.L., COEZY, E. & ROCHEFORT, H. (1982). Mode of action of LN-1643 (a triphenylbromo-ethylene antiestrogen) probable mediation by the estrogen receptor and high affinity metabolite. Biochem. Pharmac., 31, 3187–3191.CrossRefGoogle Scholar
- JORDAN, V.C. (1984). Biochemical pharmacology of antiestrogen action. Pharmac. Reviews (in press).Google Scholar
- JORDAN, V.C., HALDEMANN, B. & ALLEN, K.E. (1981). Geometric isomers of substituted triphenylethylenes and antiestrogen action. Endocrinology, 108, 1353–1361.PubMedCrossRefGoogle Scholar
- JORDAN, V.C. & LIEBERMAN, M.E. (1984). Estrogenstimulated prolactin synthesis in vitro: classification of agonists, partial agonist and antagonist actions based on structure. Mol. Pharmac. (in press).Google Scholar
- KASSIS, J.A., SAKAI, D., WALENT, J.H. & GORSKI, J. (1984). Primary cultures of estrogen-responsive cells from rat uteri: induction of progesterone receptors and a secreted protein. Endocrinology, 114, 1558–1566.PubMedCrossRefGoogle Scholar
- LIEBERMAN, M.E., GORSKI, J. & JORDAN, V.C. (1983). An estrogen receptor model to describe the regulation of prolactin synthesis by antiestrogens in vitro. J. biol. Chem., 258, 4741–4745.PubMedGoogle Scholar
- LIEBERMAN, M.E., JORDAN, V.C., FRITSCH, M., SANTOS, M.A. & GORSKI, J. (1983). Direct and reversible inhibition of estradiol-stimulated prolactin synthesis by antiestrogens in vitro. J. biol Chem., 258, 4734–4740.PubMedGoogle Scholar
- ROBERTSON, D.W., KATZENELLENBOGEN, J.A., HAYES, J.R. & KATZENELLENBOGEN, B.S. (1982). Antiestrogen basicity-activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogues of (Z)-1,2 diphenyl-1-[4-[2-(dimethylamino)ethoxy]-1-butene (tamoxifen, Nolvadex®) having altered basicity. J. med. Chem., 25, 167–171.PubMedCrossRefGoogle Scholar
- SUTHERLAND, R.L. & JORDAN, V.C. (1981). Non-steroidal antioestrogens: molecular pharmacology and antitumour actions. Sydney: Academic Press.Google Scholar
- TATE, A.C., GREENE, G.L., DeSOMBRE, E.R., JENSEN, E.V. & JORDAN, V.C. (1984). Differences between estrogen-and antiestrogen-estrogen receptor complexes from human breast tumors identified with an antibody raised against the estrogen receptor. Cancer Res., 44, 1012–1018.PubMedGoogle Scholar
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