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.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
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.
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.
JORDAN, V.C. (1984). Biochemical pharmacology of antiestrogen action. Pharmac. Reviews (in press).
JORDAN, V.C., HALDEMANN, B. & ALLEN, K.E. (1981). Geometric isomers of substituted triphenylethylenes and antiestrogen action. Endocrinology, 108, 1353–1361.
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).
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.
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.
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.
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.
SUTHERLAND, R.L. & JORDAN, V.C. (1981). Non-steroidal antioestrogens: molecular pharmacology and antitumour actions. Sydney: Academic Press.
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.
Author information
Authors and Affiliations
Editor information
Copyright information
© 1984 Macmillan Publishers Limited
About this chapter
Cite this chapter
Jordan, V.C., Koch, R., Lieberman, M.E., Mittal, S. (1984). Unexpected oestrogenic activity in a derivative of antioestrogenic triphenylethylenes. In: Paton, W., Mitchell, J., Turner, P., Padgham, C., Ashcroft, E. (eds) IUPHAR 9th International Congress of Pharmacology London 1984. Palgrave Macmillan, London. https://doi.org/10.1007/978-1-349-17615-1_13
Download citation
DOI: https://doi.org/10.1007/978-1-349-17615-1_13
Publisher Name: Palgrave Macmillan, London
Print ISBN: 978-0-333-37136-7
Online ISBN: 978-1-349-17615-1
eBook Packages: Biomedical and Life SciencesBiomedical and Life Sciences (R0)