ERA-45
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.
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| Drug class | Estrogen; Selective ERα agonist |
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See also edit
References edit
- ^ a b c d e f 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.
- ^ a b Jeanes HL, Tabor C, Black D, Ederveen A, Gray GA (2008). "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. doi:10.1677/JOE-08-0071. PMC 2386536. PMID 18492815.
- ^ Evers NM, van den Berg JH, Wang S, Melchers D, Houtman R, de Haan LH, Ederveen AG, Groten JP, Rietjens IM (2014). "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. doi:10.1016/j.jsbmb.2014.06.002. PMID 24923734. S2CID 9884692.
- ^ Khalil RA (2013). "Estrogen, vascular estrogen receptor and hormone therapy in postmenopausal vascular disease". Biochem. Pharmacol. 86 (12): 1627–42. doi:10.1016/j.bcp.2013.09.024. PMC 3840081. PMID 24099797.
- ^ a b 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.