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Research Article

Kinetic Analysis of Estrogen and Antiestrogen Competition for Hypothalamic Cytosol Estrogen Receptors. Evidence for Noncompetitive Ligand-Receptor Interactions

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Pages 531-553 | Published online: 26 Sep 2008

References

  • Wyss R. H., Karsznia R., Heinrichs W. L.-R, Herrmann W. L. Inhibition of uterine receptor binding of estradiol by anti-estrogens (Clomiphene and CL-868). J. Clin. Endocrinol. 1968; 28: 1824
  • Kahwanago I., Heinrichs W. R., Herrmann W. L. Estradiol “receptors” in hypothalamus and anterior pituitary gland: Inhibition of estradiol binding by SH-group blocking agents and clomiphene citrate. Endocrinology 1970; 86: 1319
  • Korenman S. G. Relation between estrogen inhibitory activity and binding to cytosol of rabbit and human uterus. Endocrinology 1970; 87: 1119
  • Cidlowski J. A., Muldoon T. G. Sex-related differences in the regulation of cytoplasmic estrogen receptor levels in responsive tissues of the rat. Endocrinology 1976; 98: 833
  • Jordan V. C., Dowse L. J. Tamoxifen as an anti-tumor agent: Effect on oestrogen binding. J. Endocrinology 1976; 68: 297
  • Kurl R. N., Morris I. D. Differential depletion of cytoplasmic high affinity oestrogen receptors after the in vivo administration of the antioestrogens, clomiphene, MER-25 and tamoxifen. Br. J. Pharmacol. 1978; 62: 387
  • Rochefort H., Capony F. Binding properties of an antiestrogen to the estradiol receptor of uterine cytosol. FEBS Lett. 1972; 20: 11
  • Rochefort H., Lignon F., Capony F. Effects of antiestrogens on uterine estradiol receptors. Gynec. Invest. 1972; 3: 43
  • Katzenellenbogen B. S., Katzenellenbogen J. A., Ferguson E. R., Krauthammer N. Antiestrogen interaction with uterine estrogen receptors: Studies with a radiolabeled antiestrogen (CI-628). J. Biol. Chem. 1978; 253: 697
  • Jordan V. C., Prestwich G. Binding of 3H-tamoxifen in rat uterine cytosols: A comparison of swinging bucket and vertical tube rotor sucrose density gradient analysis. Mol. Cell Endocrinol. 1977; 8: 179
  • Capony F., Rochefort H. High-affinity binding of the antiestrogen 3H-tamoxifen to the 8S estradiol receptor. Mol. Cell Endocrinol. 1978; 11: 181
  • Terenius L., Ljungkvist I. Aspects on the mode of action of antiestrogens and antiprogesterone. Gynec. Invest. 1972; 3: 96
  • Etgen A. M. Antiestrogens: Effects of tamoxifen, nafoxidine and CI-628 on sexual behavior, cytoplasmic receptors and nuclear binding of estrogen. Horm. Behav. 1979; 13: 97
  • Terenius L. Structure-activity relationship of antiestrogens with regard to interaction with 17β-estradiol in the uterus and vagina. Acta Endocrinol. 1971; 66: 431
  • Geynet C., Millet C., Truong H., Baulieu E. -E. Estrogens and antiestrogens. Gynec. Invest. 1972; 3: 2
  • Hahnel R., Twaddle E., Ratajczak T. The influence of synthetic antiestrogens on the binding of tritiated estradiol-17β by cytosols of human uterus and human breast carcinoma. J. Steroid Biochem. 1973; 4: 687
  • Goldstein A., Aronow L., Kalman S. M. Principles of Drug Action: The Basis of Pharmacology. John Wiley and Sons, New York 1974
  • van den Brink F. G. General theory of drug-receptor interactions. Kinetics of Drug Action, J. M. van Rossum. Springer-Verlag, New York 1974; 169
  • McDonald P. G. The effect of hypothalamic stimulation and progesterone on ovulation in female rats treated with the oestrogen antagonist ICI 46,474. Acta Endocrinol. 1973; 72: 345
  • Roy E. J., Wade G. M. Binding of 3H-estradiol by brain cell nuclei and female rat sexual behavior: Inhibition by antiestrogens. Brain Res. 1977; 126: 73
  • Wade G. M., Blaustein J. D. Effects of an antiestrogen on neural estradiol binding and on behaviors in female rats. Endocrinology 1978; 102: 245
  • Etgen A. M., Whalen R. E. In vitro interactions of estradiol and two antiestrogens with cytoplasmic estrogen receptors from female rat hypothalamus. Society for Neuroscience Abstracts 1979; 5: 1502
  • Ginsburg M., Greenstein B. D., MacLusky N. J., Morris I. D., Thomas P. J. An improved method for the study of highaffinity steroid binding: Oestradiol binding in brain and pituitary. Steroids 1974; 6: 773
  • Rosner A. L., Schwartz A. M., Bray C. L., Burstein N. A. Accelerated dissociation of estrogen receptor-ligand complexes by estradiol. Evidence for negative cooperativity of binding. Arch. Biochem. Biophys. 1979; 198: 153
  • Walker W. A., Feder H. H. Long-term effects of estrogen action are crucial for the display of lordosis in female guinea pigs: Antagonism by antiestrogens and correlations with in vitro cytoplasmic binding activity. Endocrinology 1979; 104: 89
  • Skidmore J. R., Walpole A. L., Woodburn J. Effect of some triphenylethylenes on oestradiol binding in vitro to macromolecules from uterus and anterior pituitary. J. Endocrinology 1974; 25: 289
  • Jordan V. C., Dix C. J., Rowsby L., Prestwich G. Studies on the mechanisms of action of the nonsteroldal anti-oestrogen tamoxifen (I.C.I. 46,474) in the rat. Mol. Cell. Endocrinol. 1977; 7: 177
  • Sutherland R. L., Murphy L. C., Foo M. S., Green M. D., Whybourne A. M., Kroowski Z. S. High-affinity antioestrogen binding site distinct from the oestrogen receptor. Nature 1980; 288: 273
  • Sherman M. R. A combined steric and allosteric model of hormone-receptor interactions. In Proceedings, Fifth Intl. Congress of Endocrinology, Hamburg, 1976. Intl. Congress Series, V. H.T. James. Excerpta Medica, Amsterdam 1977; Vol. 402: 572
  • Bullock L. P., Bardin C. W., Sherman M. R. Androgenic, anti-androgenic, and synandrogenic actions of progestins: Role of steric and allosteric interactions with androgen receptors. Endocrinology 1978; 103: 1768
  • Samuels H. H., Tomkins G. M. Relation of steroid structure to enzyme induction in hepatoma tissue culture cells. J. Mol. Biol. 1970; 52: 57
  • Suthers M. B., Pressley L. A., Funder J. W. Glucocorticoid receptors: Evidence for a second, non-glucocorticoid binding site. Endocrinology 1976; 99: 260
  • Watson G. H., Korach K. S., Muldoon T. G. Obstruction of estrogen-receptor complex formation. Further analysis of the nature and steroidal specificity of the effect. Endocrinology 1977; 101: 1733
  • Jordan V. C., Rowsby L., Dix C. J., Prestwich G. Doserelated effects of non-steroidal antioestrogens and oestrogens on the measurement of cytoplasmic oestrogen receptors in the rat and mouse uterus. J. Endocrinology 1978; 78: 71
  • Gardner R. M., Kirkland J. L., Stancel G. M. Selective blockade of estrogen-induced uterine responses by the antiestrogen nafoxidine. Endocrinology 1978; 103: 1583
  • Clark J. H., Eriksson H. A., Hardin J. W. Uterine receptorestradiol complexes and their interaction with nuclear binding sites. J. Steroid Biochem. 1976; 7: 1039
  • Clark J. H., Peck E. J., Jr. Nuclear retention of receptoroestrogen complex and nuclear acceptor sites. Nature 1976; 260: 635
  • Baudendistel L. J., Ruh T. S. Antiestrogen action: Differential nuclear retention and extractability of the estrogen receptor. Steroids 1976; 28: 223
  • Ruh T. S., Baudendistel L. J. Different nuclear binding sites for antiestrogen and estrogen receptor complexes. Endocrinology 1977; 100: 420
  • Ruh T. S., Baudendistel. Antiestrogen modulation of the salt-resistant nuclear estrogen receptor. Endocrinology 1978; 102: 1838
  • Roy E. J. Antiestrogens and nuclear estrogen receptors in the brain. Current Studies of Hypothalamic Function 1978, K. Lederis, W. L. Veale. Karger, Basel 1978; Vol. 1: 204
  • Roy E. J., McEwen B. S. An exchange assay for estrogen receptors in cell nuclei of the adult rat brain. Steroids 1977; 30: 657
  • Arai Y., Gorski R. A. Effect of antiestrogen on steroid induced sexual receptivity in ovariectomized rats. Physiol. Behav. 1968; 3: 351
  • Roy E. J., Wade G. N. Estrogenic effects of an antiestrogen, MER-25, on eating and body weight in rats. J. Comp. Physiol. Psychol. 1976; 90: 156
  • Roy E. J., Wade G. N. Role of food intake in estradiolinduced body weight changes in female rats. Horm. Behav. 1977; 8: 265
  • Mendenhall D. W., Kobayashi H., Shih F. M.L., Sternson L. A., Higushi T., Fabian C. Clinical analysis of tamoxifen, an anti-neoplastic agent, in plasma. Clin. Chem. 1978; 24: 1518
  • Borgna J. -L., Rochefort H. Occupation in vivo des recepteurs oestrogenes par des metabolites hydroxyles du tamoxifene. C.R. Acad. Sci. (Paris) 1979; 289: 1141

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