Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

ERB-26

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
ERB-26
Clinical data
Drug classEstrogen; Selective ERβ agonist

ERB-26 is asyntheticestrogen and aselectiveagonist of theERβ.[1][2] It is theactiveenantiomer of theracemic mixtureERB-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 fortransactivation of the ERβ relative to the ERα.[1] ItsEC50 value for the ERβ is 0.21 nM (4-fold weaker thanestradiol) and for the ERα is 260 nM (10,000-fold weaker than estradiol).[1] It has noantagonistic activity at either receptor.[1] ERB-26 is active in prevention ofprostate cancer development inpreclinicalmodels.[1] In contrast to ERB-26, the selective ERα agonistERA-45 induced prostate cancer development in preclinical models when it was given in combination withtestosterone, whereas testosterone alone did not do so.[1] These findings suggest opposing roles of the ERα and ERβ in theprostate gland.[1] Thechemical structure of ERB-26 does not appear to have been disclosed.

See also

[edit]

References

[edit]
  1. ^abcdefghAttia 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.


ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown


Stub icon

Thisdrug article relating to thegenito-urinary system is astub. You can help Wikipedia byadding missing information.

Retrieved from "https://en.wikipedia.org/w/index.php?title=ERB-26&oldid=1324732360"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2026 Movatter.jp