| 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
- ^ a b c d e f g h 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.
- ^ 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.
- ^ 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 drug article relating to the genito-urinary system is a stub. You can help Wikipedia by expanding it. |
| 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
- ^ a b c d e f g h 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.
- ^ 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.
- ^ 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.
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| This drug article relating to the genito-urinary system is a stub. You can help Wikipedia by expanding it. |