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Molecular mechanism of RU 486 action: a review

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References

  1. Philibert D, Deraedt R, Teutsch G: RU 38486: A potent antiglucocorticoid in vitro. (Abstr.) 8th International Congress of Pharmacology 14631, 1981

  2. Nieman L, Loriaux D: Clinical applications of the glucocorticoid and progestin antagonist RU 486. In: Receptor mediated antisteroid action, edited by Agarwal, MK, Walter de Gruyter, New York, 1987, pp 77–97

    Google Scholar 

  3. Kalimi M: Role of antiglucocorticoid RU 486 on dexamethasoneinduced hypertension in rats. Am J Physiol 256: 682–685, 1989

    Google Scholar 

  4. Kalimi M: Receptor-mediated antiprogestin action of RU 486. In: Receptor mediated antisteroid action, edited by Agarwal, MK, Walter de Gruyter, New York, 1987, pp 121–137

    Google Scholar 

  5. Heikinheimo O, Ylikorkala O, Lahteenmaki P: Antiprogesterone RU 486 - a drug for non-surgical abortion. Ann Med 22: 75–84, 1990

    Google Scholar 

  6. Permezel M: The antiprogesterone steroid, RU 486 (mifepristone). Aust NZJ Obstet Gynaecol 30: 77–80, 1990

    Google Scholar 

  7. Ulmann A, Teutsch G, Philibert D: RU 486. Sci Am 262: 42–48, 1990

    Google Scholar 

  8. Regelson W, Loria R, Kalimi M: Beyond abortion: RU 486 and the needs of the crisis constituency. JAMA 264: 1026–1027, 1990

    Google Scholar 

  9. Jung-Testas I, Baulieu EE: Antisteroid action in cultured L-29 mouse fibroblasts. J Steroid Biochem 20: 301–306, 1984

    Google Scholar 

  10. Moguilewsky M, Philibert D: RU 38486: Potent antiglucocorticoid activity correlated with strong binding to the cytosolic glucocorticoid receptors followed by an impaired activation. J Steriod Biochem 20: 271–276, 1984

    Google Scholar 

  11. Agarwal M, Lazer G: Analysis of the structure and function of steroid receptors with the aid of the antihormone RU 486. In: Receptor mediated antisteroid action, edited by Agarwal, MK Walter de Gruyter, New York, 1987, pp 43–75

    Google Scholar 

  12. Shi W, Zhu P: Autoradiographic localization of [3H]RU 486 and [3H]progesterone in the uterus, pituitary and hypothalamus of the rat. Hum Reprod 5: 505–509, 1990

    Google Scholar 

  13. Geier A, Bella R, Beery R, Lunenfeld B: Comparison of the physical properties of the nuclear progesterone receptor bound to antiprogestin RU 486 or progestin ORG 2058, following limited proteolysis. Steroids 55: 283–288, 1990

    Google Scholar 

  14. Moudgil V, Lombardo G, Hurd C, Eliezer N, Agarwal M: Evidence for separate binding sites for progesterone and RU 486 in the chick oviduct. Biochem Biophys Acta 889: 192–199, 1986

    Google Scholar 

  15. Kalimi M, Agarwal M: Interaction of antiglucocorticoid RU 486 with rat kidney glucocorticoid receptor. Biochem Biophys Res Commun 153: 365–371, 1988

    Google Scholar 

  16. Moudgil V, Jo Anter M, Hurd C: Mammalian progesterone receptor shows differential sensitivity to sulfhydryl group modifying agents when bound to agonist and antagonist ligands. J Biol Chem 264: 2203–2211, 1989

    Google Scholar 

  17. Housley P, Pratt W: Direct demonstration of glucocorticoid receptor phosphorylation by intact L-cells. J Biol Chem 258: 4630–4635, 1983

    Google Scholar 

  18. Orti E, Mendel D, Smith L, Munck A: Agonist-dependent phosphorylation and nuclear dephosphorylation of glucocorticoid receptors in intact cells. J Biol Chem 264: 9728–9731, 1989

    Google Scholar 

  19. Hoeck W, Rusconi S, Groner B: Down-regulation and phosphorylation of glucocorticoid receptors in cultured cells. Investigations with a monospecific antiserum against a bacterially expressed receptor fragment. J Biol Chem 264: 14396–14402, 1989

    Google Scholar 

  20. Rauch M, Loosfelt H, Philibert D, Milgrom E: Mechanism of action of an antiprogesterone, RU 486, in the rabbit endometrium: effects of RU 486 on the progesterone receptor and on the expression of the uteroglobin gene. Eur J Biochem 148: 213–218, 1985

    Google Scholar 

  21. Horowitz K: The antiprogestin RU 38486: Receptor-mediated progestin versus antiprogestin actions screened in estrogen-insensitive T47Dco human breast cancer cells. Endocrinology 116: 2236–2245, 1985

    Google Scholar 

  22. Moguilewsky M, Philibert D: In: The antiprogestin steroid RU 486 and fertility control, edited by Segal S, Baulieu EE, New York, Plenum Press, 1986, pp 99

  23. Lefebvre P, Formstecher P, Richard C, Dautrevaux M: RU 486 stabilizes a high molecular weight form of the glucocorticoid receptor containing the 90K non-steroid binding protein in intact thymus cells. Biochem Biophys Res Commun 150: 1221–1229, 1988

    Google Scholar 

  24. Formstecher P, Lefebvre P, Dautrevaux M: RU 486 stabilizes the glucocorticoid receptor in a non-transformed high molecular weight form in intact thymus cells under physiological conditions. J Steroid Biochem 31: 607–612, 1988

    Google Scholar 

  25. Lefebvre P, Danze P, Sablonniere B, Richard C, Formstecher P, Dautrevaux M: Association of the glucocorticoid receptor binding subunit with the 90K nonsteroid binding- component is stabi lized by both steroidal and nonsteroidal antiglucocorticoids in intact cells. Biochem 27: 9186–9194, 1988

    Google Scholar 

  26. Groyer G, Cadepond F, Groyer A, Idziorek T, Mariller M, Baulieu E: Stimulation of specific transcription and DNA binding studies suggest that in vitro transformed UR 486-glucocorticosteroid receptor complexes display agonist activity. J Steroid Biochem 30: 291–294, 1988

    Google Scholar 

  27. Groyer A, Schweizer Groyer G, Cadepond F, Mariller M, Baulieu E: Antiglucocorticosteroid effects suggest why steroid hormone is required for receptors to bind DNA in vivo but not in vitro. Nature 328: 624–626, 1987

    Google Scholar 

  28. Willmann T, Beato M: Steroid-free glucocorticoid receptor binds specifically to mouse mammary tumor virus DNA. Nature 324: 688–691, 1986

    Google Scholar 

  29. Baulieu E: Antihormone-steroid hormonal activity, heat-shock protein hsp90 and receptors. Horm Res 28: 181–195, 1987

    Google Scholar 

  30. Segnitz B, Gehring U: Mechanism of action of a steroidal antiglucocorticoid in lymphoid cells. J Biol Chem 265: 2789–2796, 1990

    Google Scholar 

  31. Lindemeyer R, Robertson N, Litwack G: Glucocorticoid receptor monoclonal antibodies define the biological action of RU 38486 in intact B16 melanoma cell. Cancer Res 50: 7985–7991, 1990

    Google Scholar 

  32. Qi M, Stasenko L, Defranco D: Recycling and desensitization of glucocorticoid receptor in V-mos transformed cells depend on the ability of nuclear receptors to modulate gene expression. Mol Endocrinology 4: 455–464, 1990

    Google Scholar 

  33. Beato M: Gene regulation by steroid hormone. Cell 56: 335–344, 1989

    Google Scholar 

  34. Kuhnel B, Al Ashry D, Edwards D, Nordeen S: Mapping contacts between unpurified human progesterone receptor and the hormone response element of mouse mammary tumor virus. DNA 8: 703–713, 1989

    Google Scholar 

  35. Hendry L: Stereochemical complementary of DNA and steroid agonists and antagonists. J Steroid Biochem 31: 493–523, 1988

    Google Scholar 

  36. Al Ashry D, Onate SA, Nordeen SK, Edwards DP: Human progesterone receptor complexed with the antagonist RU 486 binding to hormone response elements in a structurally altered form. Mol Endocrinology 3: 1545–1558, 1989

    Google Scholar 

  37. Kalff M, Gross B, Beato M: Progesteone receptor stimulates transcription of mouse mammary tumor virus in a cell-free system. Nature 344: 360–362, 1991

    Google Scholar 

  38. Schmidt T: Comparison of in vivo activation of triamcinolone acetonide and RU 38486 receptor complexes in the CEM-C7 and IM-9 human leukemic cell lines. Cancer Res 49: 4390–4395, 1989

    Google Scholar 

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Authors and Affiliations

  1. Department of Physiology, Medical College of Virginia, Virginia Commonwealth University, 23298, Richmond, Virginia, USA

    Jianren Mao, William Regelson & Mohammed Kalimi

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  1. Jianren Mao
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  2. William Regelson
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  3. Mohammed Kalimi
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Mao, J., Regelson, W. & Kalimi, M. Molecular mechanism of RU 486 action: a review. Mol Cell Biochem 109, 1–8 (1992). https://doi.org/10.1007/BF00230867

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