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Chemical Compound Review

Promestone     (8S,13S,14S,17S)-13,17- dimethyl-17...

Synonyms: Surgestone, Promegastone, Promegestone, RU-5020, RU5020, ...
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Disease relevance of Promegestone


High impact information on Promegestone

  • [(3)H]Promegestone crosslinking to TAT-CRAC could be displaced by cholesterol and promegestone, with IC50 values of 1 and 200 microM, respectively [6].
  • For AChRs in the presence of agonist (desensitized state) promegestone was a more potent inhibitor of the binding of the noncompetitive antagonist [3H]phencyclidine (IC50 = 9 microM) than of [3H]histrionicotoxin (IC50 approximately 100 microM) [7].
  • Between 1-30 microM promegestone produced a concentration-dependent enhancement of the equilibrium binding affinity of [3H]ACh to Torpedo AChR-rich membranes [7].
  • In vitro cultures of proliferative endometrium treated with the synthetic progestagen R 5020 or with RU 486 also had increased E2-DH activity; RU 486 counteracted R 5020 effects [8].
  • In T47DCO cells, 10(-8) M DMA and other 19-norandrogens stimulated transcription of a progestin/glucocorticoid/androgen response element-thymidine kinase-luciferase reporter plasmid to the same extent as R5020, the potent progestin promegestone (EC50, approximately 10(-9) M), but C-19 androgens had no effect [9].

Chemical compound and disease context of Promegestone


Biological context of Promegestone


Anatomical context of Promegestone


Associations of Promegestone with other chemical compounds


Gene context of Promegestone


Analytical, diagnostic and therapeutic context of Promegestone


  1. Transformation of estrone and estradiol in hormone-dependent and hormone-independent human breast cancer cells. Effects of the antiestrogen ICI 164,384, danazol, and promegestone (R-5020). Nguyen, B.L., Chetrite, G., Pasqualini, J.R. Breast Cancer Res. Treat. (1995) [Pubmed]
  2. One year comparison between two add-back therapies in patients treated with a GnRH agonist for symptomatic endometriosis: a randomized double-blind trial. Fernandez, H., Lucas, C., Hédon, B., Meyer, J.L., Mayenga, J.M., Roux, C. Hum. Reprod. (2004) [Pubmed]
  3. Regulation of expression of the retinoic acid metabolizing enzyme CYP26A1 in uteri of ovariectomized mice after treatment with ovarian steroid hormones. Fritzsche, B., Vermot, J., Neumann, U., Schmidt, A., Schweigert, F.J., Doll??, P., R??hl, R. Mol. Reprod. Dev. (2007) [Pubmed]
  4. Hypothalamic sites of progestin action on aggression and sexual behavior in female Syrian hamsters. Meisel, R.L., Fraile, I.G., Pfaff, D.W. Physiol. Behav. (1990) [Pubmed]
  5. Estrogen and progestin receptors in meningiomas: clinicopathological correlations. Markwalder, T.M., Markwalder, R.V., Zava, D.T. Clinical neuropharmacology. (1984) [Pubmed]
  6. Cholesterol binding at the cholesterol recognition/ interaction amino acid consensus (CRAC) of the peripheral-type benzodiazepine receptor and inhibition of steroidogenesis by an HIV TAT-CRAC peptide. Li, H., Yao, Z., Degenhardt, B., Teper, G., Papadopoulos, V. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  7. The steroid promegestone is a noncompetitive antagonist of the Torpedo nicotinic acetylcholine receptor that interacts with the lipid-protein interface. Blanton, M.P., Xie, Y., Dangott, L.J., Cohen, J.B. Mol. Pharmacol. (1999) [Pubmed]
  8. Endometrial and pituitary responses to the steroidal antiprogestin RU 486 in postmenopausal women. Gravanis, A., Schaison, G., George, M., de Brux, J., Satyaswaroop, P.G., Baulieu, E.E., Robel, P. J. Clin. Endocrinol. Metab. (1985) [Pubmed]
  9. Dimethandrolone undecanoate: a new potent orally active androgen with progestational activity. Attardi, B.J., Hild, S.A., Reel, J.R. Endocrinology (2006) [Pubmed]
  10. Estrone sulfate-sulfatase and 17 beta-hydroxysteroid dehydrogenase activities: a hypothesis for their role in the evolution of human breast cancer from hormone-dependence to hormone-independence. Pasqualini, J.R., Chetrite, G., Nguyen, B.L., Maloche, C., Delalonde, L., Talbi, M., Feinstein, M.C., Blacker, C., Botella, J., Paris, J. J. Steroid Biochem. Mol. Biol. (1995) [Pubmed]
  11. Human estrogen sulfotransferase (hEST1) activities and its mRNA in various breast cancer cell lines. Effect of the progestin, promegestone (R-5020). Chetrite, G., Le Nestour, E., Pasqualini, J.R. J. Steroid Biochem. Mol. Biol. (1998) [Pubmed]
  12. Biological effects of progestins in breast cancer. Pasqualini, J.R., Ebert, C., Chetrite, G.S. Gynecol. Endocrinol. (2001) [Pubmed]
  13. Role, control and expression of estrone sulfatase and 17 beta-hydroxysteroid dehydrogenase activities in human breast cancer. Pasqualini, J.R. Zentralblatt für Gynäkologie. (1997) [Pubmed]
  14. Progesterone receptor in the chick bursa of fabricius: characterization and immunohistochemical localization. Ylikomi, T., Gasc, J.M., Isola, J., Baulieu, E.E., Tuohimaa, P. Endocrinology (1985) [Pubmed]
  15. Non-classical antiestrogenic actions of dexamethasone in variant MCF-7 human breast cancer cells in culture. Zhou, F., Bouillard, B., Pharaboz-Joly, M.O., André, J. Mol. Cell. Endocrinol. (1989) [Pubmed]
  16. Progesterone and promegestone stimulate human bone cell proliferation and insulin-like growth factor-2 production. Tremollieres, F.A., Strong, D.D., Baylink, D.J., Mohan, S. Acta Endocrinol. (1992) [Pubmed]
  17. Active immunization of female rats against 17 beta-estradiol. Preliminary studies on 17 beta-estradiol binding in uterine and pituitary cytosols. Samperez, S., Bourtourault, M., Rault, B., Jouan, P. J. Steroid Biochem. (1983) [Pubmed]
  18. Progesterone receptors in rat thymus. Pearce, P.T., Khalid, B.A., Funder, J.W. Endocrinology (1983) [Pubmed]
  19. Zinc concentration and progestin receptor in human benign hyperplastic prostate. Imai, K., Schneider, S.L., Drury, R.E., Murphy, G.P., Sandberg, A.A. J. Urol. (1984) [Pubmed]
  20. Nongenomic inhibition of oxytocin binding by progesterone in the ovine uterus. Dunlap, K.A., Stormshak, F. Biol. Reprod. (2004) [Pubmed]
  21. Differential effects of catechol estrogens, progestins and CI-628 administered by constant infusion on the central and peripheral action of estradiol. Jellinck, P.H., Luine, V., McEwen, B.S. Neuroendocrinology (1982) [Pubmed]
  22. Effects of progestins and antiprogestins on mitochondria in uterine glandular cells in the rat. A quantitative investigation. Secchi, J., Lecaque, D. Cell Tissue Res. (1984) [Pubmed]
  23. Molecular cloning, sequence analyses, and expression of complementary DNA encoding murine progesterone receptor. Schott, D.R., Shyamala, G., Schneider, W., Parry, G. Biochemistry (1991) [Pubmed]
  24. The metabolic clearance rate, the brain extraction and distribution and the uterine extraction and retention of progesterone and R 5020 in estrogen-treated ovariectomized rabbits. Rahman, S.S., Billiar, R.B., Miguel, R., Johnson, W., Little, B. Endocrinology (1977) [Pubmed]
  25. Recent insight on the control of enzymes involved in estrogen formation and transformation in human breast cancer. Pasqualini, J.R., Chetrite, G.S. J. Steroid Biochem. Mol. Biol. (2005) [Pubmed]
  26. The selective estrogen enzyme modulator (SEEM) in breast cancer. Chetrite, G.S., Pasqualini, J.R. J. Steroid Biochem. Mol. Biol. (2001) [Pubmed]
  27. Inhibition of growth and induction of apoptosis by androgens of a variant of LNCaP cell line. Joly-Pharaboz, M.O., Ruffion, A., Roch, A., Michel-Calemard, L., André, J., Chantepie, J., Nicolas, B., Panaye, G. J. Steroid Biochem. Mol. Biol. (2000) [Pubmed]
  28. Immunocytochemical determination of estrogen and progesterone receptors in human endometrial adenocarcinoma cells (Ishikawa cells). Hata, H., Kuramoto, H. J. Steroid Biochem. Mol. Biol. (1992) [Pubmed]
  29. Interactions of oestradiol benzoate and promegestone upon basal and TRH-induced prolactin secretion in postmenopausal women. Joseph, P.J., Couzinet, B., Brailly, S., Rigaud, C., Raynaud, J.P., Schaison, G. Clin. Endocrinol. (Oxf) (1986) [Pubmed]
  30. Endometrial integrin expression is independent of estrogen or progestin treatment in vitro. Sillem, M., Prifti, S., Schmidt, M., Rabe, T., Runnebaum, B. Fertil. Steril. (1997) [Pubmed]
  31. Effects of estradiol and promegestone on human breast cell cultures. An ultrastructural study. Chomette, G., Auriol, M., Tranbaloc, P., Gompel, A., Malet, C., Kuttenn, F. Pathol. Res. Pract. (1986) [Pubmed]
  32. Progesterone receptor quantification with radiolabeled promegestone (R 5020) in frozen sections of endometrium and breast cancer tissue. De Goeij, A.F., Scheres, H.M., Rousch, M.J., Hondius, G.G., Bosman, F.T. J. Steroid Biochem. (1988) [Pubmed]
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