Estrone sulfate

E1S itself is biologically inactive, with less than 1% of the relative binding affinity of estradiol for the ERα and ERβ.

[5] Simultaneously, estrogen sulfotransferases, including SULT1A1 and SULT1E1, convert estrone to E1S, resulting in an equilibrium between the two steroids in various tissues.

[1][6][7] In accordance, E1S has been found to transactivate the estrogen receptor at physiologically relevant concentrations.

[8][9] Unlike unconjugated estradiol and estrone, which are lipophilic compounds, E1S is an anion and is hydrophilic.

[24][25] Studies in animals and humans have had mixed findings on uptake of exogenously administered E1S in normal and tumorous mammary gland tissue.

[26][27][28][24][25] This is in contrast to substantial uptake of exogenously administered estradiol and estrone by the mammary glands.

[26] Another animal study found that E1S wasn't taken up by the uterus but was taken up by the liver, where it was hydrolyzed into estrone.

Skeletal formula of estrone sulfate
Space-filling model of the estrone sulfate molecule
Estrogen levels with radioimmunoassay (RIA) around mid-cycle during the normal menstrual cycle in women. [ 32 ] [ 33 ] The vertical dashed line in the center is mid-cycle.