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Etacstil

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This is an old revision of this page, as edited by Graeme Bartlett (talk | contribs) at 23:25, 25 October 2016 (added Category:Selective estrogen receptor modulators using HotCat). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Etacstil, known as, GW-5638 is a discontinued selective estrogen receptor modulator drug that was developed by Glaxo Wellcome, and later, GlaxoSmithKline for the treatment of hormone receptor-positive breast cancer.[1] [2][3] GW-5638 was shown to overcome tamoxifene-resistance in breast cancer by altering the shape of the estrogen receptor, thus exhibiting selective estrogen receptor degrader properties.[4] [5] [6] [7] [8]

References

  1. ^ Cancer Chemoprevention: Volume 2: Strategies for Cancer Chemoprevention.
  2. ^ "T GW 5638 Profile".
  3. ^ "Nuclear Receptor Signaling Atlas".
  4. ^ Antiestrogen GW5638 induces a unique structural change in the ER. The biological significance of this conformational change was revealed in studies that demonstrated that tamoxifen-resistant breast tumor explants are not cross-resistant to GW5638. Because of these properties, this drug is currently being developed as a potential therapeutic for tamoxifen-resistant breast cancers."Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational change in the estrogen receptor". Cancer Res. 2001.
  5. ^ "GW5638 uniquely alters the shape of the estrogen receptor ".
  6. ^ "Tamoxifen-like drug suggests new ways to selectively block estrogen".
  7. ^ "Effects of a new clinically relevant antiestrogen (GW5638) related to tamoxifen on breast and endometrial cancer growth in vivo". Clin Cancer Res. 2002.
  8. ^ "Quantitative comparison of the inhibitory effects of GW5638 and tamoxifen on angiogenesis in the cornea pocket assay". Angiogenesis. 2006. doi:10.1007/s10456-006-9029-x.