Английская Википедия:17α-Epiestriol

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17α-Epiestriol, or simply 17-epiestriol, also known as 16α-hydroxy-17α-estradiol or estra-1,3,5(10)-triene-3,16α,17α-triol, is a minor and weak endogenous estrogen, and the 17α-epimer of estriol (which is 16α-hydroxy-17β-estradiol).[1][2][3] It is formed from 16α-hydroxyestrone.[4][5] In contrast to other endogenous estrogens like estradiol, 17α-epiestriol is a selective agonist of the ERβ.[6] It is described as a relatively weak estrogen, which is in accordance with its relatively low affinity for the ERα.[7] 17α-Epiestriol has been found to be approximately 400-fold more potent than estradiol in inhibiting tumor necrosis factor α (TNFα)-induced vascular cell adhesion molecule 1 (VCAM-1) expression in vitro.[8]

Relative affinities (%) of 17α-epiestriol and related steroids[9][10][11][12]
Compound Шаблон:Abbrlink Шаблон:Abbrlink Шаблон:Abbrlink Шаблон:Abbrlink Шаблон:Abbrlink Шаблон:Abbrlink Шаблон:Abbrlink
Estradiol 2.6 7.9 100 0.6 0.13 8.7 <0.1
Alfatradiol <1 <1 15 <1 <1 ? ?
Estriol <1 <1 15 <1 <1 ? ?
16β-Epiestriol <1 <1 20 <1 <1 ? ?
17α-Epiestriol <1 <1 31 <1 <1 ? ?
Values are percentages (%). Reference ligands (100%) were progesterone for the Шаблон:Abbrlink, testosterone for the Шаблон:Abbrlink, [[estradiol (medication)|Шаблон:Abbr]] for the Шаблон:Abbrlink, Шаблон:Abbrlink for the Шаблон:Abbrlink, aldosterone for the Шаблон:Abbrlink, Шаблон:Abbrlink for Шаблон:Abbrlink, and cortisol for Шаблон:Abbrlink.

See also

References

Шаблон:Reflist

Шаблон:Steroid hormones Шаблон:Estrogen receptor modulators


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