Template:Affinities and estrogenic potencies of estrogen esters and ethers at the estrogen receptors: Difference between revisions
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Latest revision as of 22:39, 11 February 2025
Template:No selflink | Other names | RBA (%)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] |
File:Test Template Info-Icon - Version (2).svg Template documentation
See also
- Template:Affinities of estrogen receptor ligands for the ERα and ERβ
- Template:Relative affinities of estrogens for steroid hormone receptors and blood proteins
- Template:Selected biological properties of endogenous estrogens in rats
References
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- ↑ Lua error in Module:Citation/CS1/Configuration at line 2088: attempt to index field '?' (a nil value).
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- ↑ Lua error in Module:Citation/CS1/Configuration at line 2088: attempt to index field '?' (a nil value).
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- ↑ Lua error in Module:Citation/CS1/Configuration at line 2088: attempt to index field '?' (a nil value).
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- ↑ Lua error in Module:Citation/CS1/Configuration at line 2088: attempt to index field '?' (a nil value).