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Template:Affinities and estrogenic potencies of estrogen esters and ethers at the estrogen receptors

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Affinities and estrogenic potencies of estrogen esters and ethers at the estrogen receptors
Template:No selflink Other names RBATooltip Relative binding affinity (%)a REP (%)b
ER ERα ERβ
Template:No selflink E2 100 100 100
Template:No selflink E2S; E2-3S ? 0.02 0.04
Template:No selflink E2-3G ? 0.02 0.09
Template:No selflink E2-17G ? 0.002 0.0002
Template:No selflink EB; Estradiol 3-benzoate 10 1.1 0.52
Template:No selflink E2-17A 31–45 24 ?
Template:No selflink EDA; Estradiol 3,17β-diacetate ? 0.79 ?
Template:No selflink EP; Estradiol 17β-propionate 19–26 2.6 ?
Template:No selflink EV; Estradiol 17β-valerate 2–11 0.04–21 ?
Template:No selflink EC; Estradiol 17β-cypionate ?c 4.0 ?
Template:No selflink Estradiol 17β-palmitate 0 ? ?
Template:No selflink Estradiol 17β-stearate 0 ? ?
Template:No selflink E1; 17-Ketoestradiol 11 5.3–38 14
Template:No selflink E1S; Estrone 3-sulfate 2 0.004 0.002
Template:No selflink E1G; Estrone 3-glucuronide ? <0.001 0.0006
Template:No selflink EE; 17α-Ethynylestradiol 100 17–150 129
Template:No selflink EE 3-methyl ether 1 1.3–8.2 0.16
Template:No selflink EE 3-cyclopentyl ether ? 0.37 ?
Footnotes: a = Relative binding affinities (RBAs) were determined via in-vitro displacement of labeled Template:No selflink from estrogen receptors (ERs) generally of rodent uterine cytosol. Estrogen esters are variably hydrolyzed into estrogens in these systems (shorter ester chain length -> greater rate of hydrolysis) and the ER RBAs of the esters decrease strongly when hydrolysis is prevented.[1][2] b = Relative estrogenic potencies (REPs) were calculated from half-maximal effective concentrations (EC50) that were determined via in-vitro β‐galactosidase (β-gal) and green fluorescent protein (GFP) production assays in yeast expressing human ERα and human ERβ. Both mammalian cells and yeast have the capacity to hydrolyze estrogen esters.[3] c = The affinities of Template:No selflink for the ERs are similar to those of Template:No selflink and Template:No selflink (figure).[4] Sources: Affinities: [1][2][5][6][7] Estrogenic potencies: [8][9][10][11] Additional: [4][3][12]
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