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ERA-45

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
ERA-45
Clinical data
Drug classEstrogen; Selective ERα agonist
Identifiers
CAS Number
PubChem SID

ERA-45 is asyntheticestrogen and aselectiveagonist of theERα.[1][2][3][4] It shows 286-foldselectivity fortransactivation of the ERα over the ERβ, withEC50 values of 0.37 nM for the ERα (7-fold weaker thanestradiol) 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 noantagonistic activity at either receptor.[1] ERA-45 induced prostate cancer development inpreclinicalmodels when it was given in combination withtestosterone, whereas testosterone alone did not do so.[1][5] In contrast, the selective ERβ agonistERB-26 was protective against the development ofprostate cancer produced by these two drugs.[1][5] These findings suggest opposing roles of the ERα and ERβ in theprostate gland.[1] Thechemical structure of ERa-45 does not appear to have been disclosed.

See also

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References

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  1. ^abcdefAttia 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. ^abJeanes 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.
  3. ^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.
  4. ^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.
  5. ^abNelson 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.


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


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