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Chemical Compound Review

AC1L3P3W     (8S,9R,13S,14S,17S)-13- methyl-11-[4-[5-(4...

Synonyms: RU 58668, RU 58 668, 151555-47-4
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Disease relevance of RU 58 668


High impact information on RU 58 668

  • No difference was observed in the fate of ER whether bound to pure antiestrogens ICI 182,780 or RU 58668 [5].
  • Interaction and dissociation by ligands of estrogen receptor and Hsp90: the antiestrogen RU 58668 induces a protein synthesis-dependent clustering of the receptor in the cytoplasm [6].
  • Thus, several biodegradable drug delivery systems containing either "mixed" (4-hydroxytamoxifen - 4-HT) or "pure" (RU 58668 - RU) AEs were prepared [7].
  • In most of multiple myeloma (MM) cells, the "pure" antiestrogen (AE) RU 58668 (RU) induced either a G1-arrest (LP-1, OPM-2, NCI-H929, U266 cells) or apoptosis (RPMI 8226 cells) [2].
  • On the other hand, we did not find that blocking estrogen receptors with RU 58668 inhibited the restoration of copulatory behavior or partner preference in testosterone-treated gonadectomized male rats, even though the level of brain nuclear estrogen receptor occupation was significantly reduced to the level found in gonadectomized males [8].

Chemical compound and disease context of RU 58 668


Biological context of RU 58 668

  • In vitro, 1 nM RU 58668 induced an accumulation of MCF-7 cells in G0/G1 phases of the cell cycle within 48 h and, in contrast to trans-4-hydroxy-tamoxifen, blocked the invasiveness of ras-transfected MCF-7 cells into the chick embryo heart during the three weeks of co-culture [1].
  • However, the kinetics of these degradations are slower than those induced by the selective estrogen receptor down-regulator RU 58668 (RU) [9].
  • Interestingly, ligands able to down-regulate ER (i.e. E2 or RU 58 668) increased ER phosphorylation while 4-OH-TAM which up-regulate the receptor had little effect in this regard [10].
  • Effects of the antiestrogen, RU 58668, on female sexual behavior in rats [3].

Anatomical context of RU 58 668

  • The known ability of these ligands to stabilize ER in the cell nucleus before regulating ER level may explain this phenomenon since such antagonism was not recorded with pure AE RU 58 668, which is known to impede nuclear translocation of the receptor [10].
  • The recently described pure antiestrogen RU 58668 displayed potent antiproliferative activities in vitro on several ER+ human mammary cell lines, stimulated either by estradiol or by endogenous or exogenous growth factors [11].

Associations of RU 58 668 with other chemical compounds


Analytical, diagnostic and therapeutic context of RU 58 668

  • Our results demonstrate that RU 58668 can reach the brain following a subcutaneous injection, but that it needs more time to reach the brain than it does to reach the pituitary [14].


  1. RU 58668: further in vitro and in vivo pharmacological data related to its antitumoral activity. Van de Velde, P., Nique, F., Planchon, P., Prévost, G., Brémaud, J., Hameau, M.C., Magnien, V., Philibert, D., Teutsch, G. J. Steroid Biochem. Mol. Biol. (1996) [Pubmed]
  2. Improved antitumoral properties of pure antiestrogen RU 58668-loaded liposomes in multiple myeloma. Maillard, S., Gauduchon, J., Marsaud, V., Gouilleux, F., Connault, E., Opolon, P., Fattal, E., Sola, B., Renoir, J.M. J. Steroid Biochem. Mol. Biol. (2006) [Pubmed]
  3. Effects of the antiestrogen, RU 58668, on female sexual behavior in rats. Vagell, M.E., McGinnis, M.Y. Brain Res. Bull. (1996) [Pubmed]
  4. Pure antiestrogen RU 58668-loaded nanospheres: morphology, cell activity and toxicity studies. Ameller, T., Marsaud, V., Legrand, P., Gref, R., Renoir, J.M. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. (2004) [Pubmed]
  5. Various phosphorylation pathways, depending on agonist and antagonist binding to endogenous estrogen receptor alpha (ERalpha), differentially affect ERalpha extractability, proteasome-mediated stability, and transcriptional activity in human breast cancer cells. Marsaud, V., Gougelet, A., Maillard, S., Renoir, J.M. Mol. Endocrinol. (2003) [Pubmed]
  6. Interaction and dissociation by ligands of estrogen receptor and Hsp90: the antiestrogen RU 58668 induces a protein synthesis-dependent clustering of the receptor in the cytoplasm. Devin-Leclerc, J., Meng, X., Delahaye, F., Leclerc, P., Baulieu, E.E., Catelli, M.G. Mol. Endocrinol. (1998) [Pubmed]
  7. Improved anti-tumoral capacity of mixed and pure anti-oestrogens in breast cancer cell xenografts after their administration by entrapment in colloidal nanosystems. Renoir, J.M., Stella, B., Ameller, T., Connault, E., Opolon, P., Marsaud, V. J. Steroid Biochem. Mol. Biol. (2006) [Pubmed]
  8. The role of gonadal steroid receptor activation in the restoration of sociosexual behavior in adult male rats. Vagell, M.E., McGinnis, M.Y. Hormones and behavior. (1998) [Pubmed]
  9. Estrogen receptor alpha and beta subtype expression and transactivation capacity are differentially affected by receptor-, hsp90- and immunophilin-ligands in human breast cancer cells. Gougelet, A., Bouclier, C., Marsaud, V., Maillard, S., Mueller, S.O., Korach, K.S., Renoir, J.M. J. Steroid Biochem. Mol. Biol. (2005) [Pubmed]
  10. Decrease of estrogen receptor expression and associated ERE-dependent transcription in MCF-7 breast cancer cells after oligomycin treatment. Seo, H.S., Journé, F., Larsimont, D., Sotiriou, C., Leclercq, G. Steroids (2003) [Pubmed]
  11. Exploration of the therapeutic potential of the antiestrogen RU 58668 in breast cancer treatment. Van de Velde, P., Nique, F., Brémaud, J., Hameau, M.C., Philibert, D., Teutsch, G. Ann. N. Y. Acad. Sci. (1995) [Pubmed]
  12. Mechanisms governing the accumulation of estrogen receptor alpha in MCF-7 breast cancer cells treated with hydroxytamoxifen and related antiestrogens. Laïos, I., Journe, F., Laurent, G., Nonclercq, D., Toillon, R.A., Seo, H.S., Leclercq, G. J. Steroid Biochem. Mol. Biol. (2003) [Pubmed]
  13. Resveratrol, a polyphenolic phytoalexin present in red wine, enhances expression and activity of endothelial nitric oxide synthase. Wallerath, T., Deckert, G., Ternes, T., Anderson, H., Li, H., Witte, K., Förstermann, U. Circulation (2002) [Pubmed]
  14. Inhibition of brain oestrogen receptors by RU 58668. Vagell, M.E., McGinnis, M.Y. J. Neuroendocrinol. (1997) [Pubmed]
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