Chemistry:ERB-26
| Clinical data | |
|---|---|
| Drug class | Estrogen; 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
- Diarylpropionitrile
- ERB-196
- Erteberel
- FERb 033
- Prinaberel (ERB-041)
- WAY-166818
- WAY-200070
- WAY-214156
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 "Opposing roles of ERα and ERβ in the genesis and progression of adenocarcinoma in the rat ventral prostate". Prostate 72 (9): 1013–22. 2012. doi:10.1002/pros.21507. PMID 22025007.
- ↑ "Estrogen receptor beta in prostate cancer: friend or foe?". Endocr. Relat. Cancer 21 (4): T219–34. 2014. doi:10.1530/ERC-13-0508. PMID 24402043.
- ↑ "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. 2010. doi:10.1186/ar3032. PMID 20497523.
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