Chemistry:ERA-45
| Clinical data | |
|---|---|
| Drug class | Estrogen; Selective ERα agonist |
| Identifiers | |
| CAS Number | |
ERA-45 is a synthetic estrogen and a selective agonist of the ERα.[1][2][3][4] It shows 286-fold selectivity for transactivation of the ERα over the ERβ, with EC50 values of 0.37 nM for the ERα (7-fold weaker than estradiol) and 13 nM for the ERβ (20,000-fold weaker than estradiol).[1] However, another found only about 35-fold potency for transactivation of the ERα over the ERβ.[2] The drug has no antagonistic activity at either receptor.[1] 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][5] In contrast, the selective ERβ agonist ERB-26 was protective against the development of prostate cancer produced by these two drugs.[1][5] These findings suggest opposing roles of the ERα and ERβ in the prostate gland.[1] The chemical structure of ERa-45 does not appear to have been disclosed.
See also
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "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.
- ↑ 2.0 2.1 "Oestrogen-mediated cardioprotection following ischaemia and reperfusion is mimicked by an oestrogen receptor (ER)α agonist and unaffected by an ER beta antagonist". J. Endocrinol. 197 (3): 493–501. 2008. doi:10.1677/JOE-08-0071. PMID 18492815.
- ↑ "Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists". J. Steroid Biochem. Mol. Biol. 143: 376–85. 2014. doi:10.1016/j.jsbmb.2014.06.002. PMID 24923734.
- ↑ "Estrogen, vascular estrogen receptor and hormone therapy in postmenopausal vascular disease". Biochem. Pharmacol. 86 (12): 1627–42. 2013. doi:10.1016/j.bcp.2013.09.024. PMID 24099797.
- ↑ 5.0 5.1 "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.
 |  |
