ERB-26
Clinical data
Drug classEstrogen; Selective ERβ agonist

ERB-26 is a synthetic estrogen and a selective agonist of the ERβ.[1][2] It is the active enantiomer of the racemic mixture ERB-79.[1] Whereas ERB-79 shows 484-fold selectivity for the ERβ over the ERα,[3] ERB-26 differs slightly in that it is even more selective, showing greater than 1,000-fold selectivity for transactivation of the ERβ relative to the ERα.[1] Its EC50 value for the ERβ is 0.21 nM (4-fold weaker than estradiol) and for the ERα is 260 nM (10,000-fold weaker than estradiol).[1] It has no antagonistic activity at either receptor.[1] ERB-26 is active in prevention of prostate cancer development in preclinical models.[1] In contrast to ERB-26, the selective ERα agonist ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testosterone alone did not do so.[1] These findings suggest opposing roles of the ERα and ERβ in the prostate gland.[1] The chemical structure of ERB-26 does not appear to have been disclosed.

See also

References

  1. 1 2 3 4 5 6 7 8 Attia DM, Ederveen AG (2012). "Opposing roles of ERα and ERβ in the genesis and progression of adenocarcinoma in the rat ventral prostate". Prostate. 72 (9): 1013–22. doi:10.1002/pros.21507. PMID 22025007. S2CID 12951793.
  2. ↑ Nelson AW, Tilley WD, Neal DE, Carroll JS (2014). "Estrogen receptor beta in prostate cancer: friend or foe?". Endocr. Relat. Cancer. 21 (4): T219–34. doi:10.1530/ERC-13-0508. PMID 24402043.
  3. ↑ Dulos J, Vijn P, van Doorn C, Hofstra CL, Veening-Griffioen D, de Graaf J, Dijcks FA, Boots AM (2010). "Suppression of the inflammatory response in experimental arthritis is mediated via estrogen receptor α but not estrogen receptor β". Arthritis Res. Ther. 12 (3): R101. doi:10.1186/ar3032. PMC 2911889. PMID 20497523.



This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.