Abstract
Estrogenic steroid hormones interact with target tissues through their binding to specific receptor proteins (1–3). Triphenylethylene derivatives inhibit several estrogen-stimulated responses, and are thus termed anti-estrogens (4–6). Triphenylethylene antiestrogens have been used effectively in the treatment of hormone-dependent cancers. MCF-7, a well established human breast cancer cell line, has been a useful tool for steroid receptor studies as these cells contain high levels of estrogen and progesterone receptors, and cell growth is inhibited markedly by antiestrogens in the absence or presence of estrogens (7–12). Current studies of antiestrogen action utilize high affinity triphenylethylene derivatives which allow a more accurate assessment of the physicochemical characteristics of receptor complexes (13–15). Although physicochemical differences in the estrogen receptor bound by estrogen versus antiestrogen have been reported by our laboratory as well as by others (16–20), it is not clear how these receptor complexes interact with nuclear binding sites which have been proposed to involve various domains such as DNA sequences, chromatin, nucleoacidic proteins and nuclear matrix (21–25). Thus, the cellular mechanisms whereby these triphenylethylene compounds provoke agonist, antagonist, and unique responses is still not clear. Antiestrogens act as mixed agonists/antagonists both in vivo and in vitro.
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
Jensen, E.V. and DeSombre, E.R. Science 182:126–134, 1973.
O’Malley, B.W. and Means, A.R. Science 183:610–620, 1974.
Gorski, J. and Gannon, F. Ann. Rev. Phys. 38:425–450, 1976.
Clark, J.H., Anderson, J.N. and Peck Jr., E.J. Steroids 22:707–718, 1973.
Katzenellenbogen, B.S. and Ferguson, E.R. Endocrinology 97:1–12, 1975.
Ruh, T.S., Baudendistel, L.J., Nicholson, W.F. and Ruh, M.F. J. Steroid Biochem. 11:315–322, 1979.
Coezy, E., Borgna, J.L. and Rochefort, H. Cancer Res. 42:317–323, 1982.
Katzenellenbogen, B.S., Norman, M.J., Eckert, R.L., Peltz, S.W. and Mangel, W.F. Cancer Res. 44:112–119, 1984.
Butler, W.B., Kirkland, W.L., Gargala, L., Goran, N., Kelsey, W.H. and Berlinske, P.J. Cancer Res. 43:1637–1644, 1983.
Horwitz, K.B., Costlow, M.E. and McGuire, W.L. Steroids 25:785–795, 1975.
Reddel, R.R., Murphy, L.C. and Sutherland, R.L. Cancer Res. 43:4618–4624, 1983.
Scholl, S.M., Huff, K.K. and Lippman, M.E. Endocrinology 113:611–617, 1983.
Borgna, J.L. and Rochefort, H. Mol. Cell. Endo. 20:71–85, 1980.
Katzenellenbogen, B.S., Pavlik, E.J., Robertson, D.W. and Katzenellenbogen, J.A. J. Biol. Chem. 256:2908–2915, 1981.
Keene, J.L., Sweet, F., Ruh, M.F. and Ruh, T.S. Biochem. J. 217:817–826, 1984.
Eckert, R.L. and Katzenellenbogen, B.S. J. Biol. Chem. 257:8840–8846, 1982.
Miller, M.A., Greene, G.L. and Katzenellenbogen, B.S. Endocrinology 114:296–298, 1984.
Evans, E., Baskevitch, P.P. and Rochefort, H. Eur. J. Biochem. 128:185–191, 1982.
Borgna, J.L., Fauque, J. and Rochefort, H. Biochemistry 23:2612–26, 1984.
Singh, R.K., Ruh, M.F. and Ruh, T.S. J. Steroid Biochem. 21:205–208, 1984.
Sun, H.K., Pfendner, E.G., Senior M.B. and Frankel, F.R. Mol. Cell. Endo. 30:267–278, 1983.
Speisberg, T.C., Webster, R., Pickler, G., Thrall, C. and Wells, D. J. Steroid Biochem. 7:1091–1101, 1976.
Thrall, C. and Speisberg, T.C. Biochemistry 19:4130–4138.
Barrack, E.R. and Coffey, D.S. Recent Prog. Horm. Res. 38:133–195, 1982.
Simmen, R.C.M., Means, A.R. and Clark J.H. Endocrinology 115:1197–1202, 1984.
Lippman, M.E., Boland, G. and Huff, K. Cancer Res. 36:4595–4601, 1976.
Horwitz, K.B., Koseki, Y. and McGuire, W.L. Endocrinology 103:1742–1751, 1978.
Ruh, T.S. and Ruh, M.F. Pharmac. Ther. 21:247–264, 1983.
Grody, W.W., Schrader, W.T. and O’Malley, B.W. Endocr. Rev. 3:141–163, 1982.
Speisberg, T.C., Steggles, A.W. and O’Malley, B.W. J. Biol. Chem. 246:4188–4197, 1971.
Miller, J.B. and Toft, D.O. Biochemistry 17:173–177, 1978.
Moudgil, V.K., Kruezak, V., Eessalu, T., Paulose, T., Taylor, M. and Hansen, J. Eur. J. Biochem. 118:547–555, 1981.
Keene, J.L., Ruh, M.F. and Ruh, T.S. J. Steroid Biochem. 21:625–631, 1984.
Jasper, T.W., Ruh, M.F. and Ruh, T.S. J. Steroid Biochem: 23:537–545, 1985.
Sheen, Y.Y., Ruh, T.S., Mangel, W.F. and Katzenellenbogen, B.S. Cancer Res. 45:4192–4199, 1985.
Compton, J.G., Schrader, W.T. and O’Malley, B.W. Biochem. Biophys. Res. Comm. 105:96–104, 1982.
Payvar, F., Wrange, O., Carlstedt-Duke, J., Okret, S., Gustafsson, J.A. and Yamamoto, K. Proc. Natl. Acad. Sci. U.S.A. 78:6628–6632, 1981.
Mulvihill, E.R., LePennec, J.P. and Chambon, P. Cell 28:621–632, 1982.
Lebeau, M.C., Massol, N. and Baulieu, E.E. Biochem. J. 204:653–662, 1982.
Spelsberg, T.C., Littlefield, B.A., Seelke, R., Martin-Dani, G., Toyoda, H., Boyd-Leinen, P., Thrall, C. and Kon, O Rec. Prog. Horm. Res. 39:464–517, 1983.
Singh, R.K., Ruh, M.F. and Ruh, T.S. Biochim. Biophys. Acta 800:33–40, 1984.
Singh, R.K., Ruh, M.F., Butler, W.B. and Ruh, T.S. Endocrinology 118:1087–1095, 1986.
Ruh, T.S. and Spelsberg, T.C. Biochem. J. 210:905–912, 1983.
Ruh, M.F., Singh, R.K., Mak, P. and Callard, G.V. Endocrinology, 118:811–818, 1986.
Ruh, T.S., Ross Jr., P., Wood, D.M. and Keene, J.L. Biochem. J. 200:133–142, 1981.
Ross Jr., P. and Ruh, T.S. Biochim. Biophys. Acta 782:18–25, 1984.
Shyamala, G., Singh, R.K., Ruh, M.F. and Ruh, T.S. Endocrinology, In Press.
Scatchard, G. Ann. N.Y. Acad. Sci. 51:660–672, 1949.
Ruh, T.S. and Baudendistel, L.J. Endocrinology 100:420–426, 1977.
Ruh, T.S. and Baudendistel, L.J. Endocrinology 102:1838–1846, 1978.
Katzenellenbogen, B. and Gorski, J. In: Biochemical Actions of Hormones, Vol. III (Ed. G. Litwack), Academic Press, New York, 1975, pp. 187–243.
Stack, G. and Gorski, J. Endocrinology 117:2024–2032, 1985.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1987 Martinus Nijhoff Publishing, Boston
About this chapter
Cite this chapter
Ruh, T.S., Ruh, M.F., Singh, R.K., Butler, W.B. (1987). Nuclear Acceptor Sites for the Mammalian Estrogen Receptor: Effects of Antiestrogens. In: Spelsberg, T.C., Kumar, R. (eds) Steroid and Sterol Hormone Action. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-2073-9_7
Download citation
DOI: https://doi.org/10.1007/978-1-4613-2073-9_7
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4612-9230-2
Online ISBN: 978-1-4613-2073-9
eBook Packages: Springer Book Archive