Target intelligence / Profile preview

Estrogen sulfotransferase (EST)

Target
EST
Molecular classification
Enzyme, Transferase, Sulfotransferase
01

Overview

Estrogen sulfotransferase (abbreviated as EST, gene symbol SULT1E1) is a cytosolic phase II conjugating enzyme that catalyzes the transfer of a sulfate group from 3′-phosphoadenosine-5′-phosphosulfate (PAPS) to the hydroxyl group of estrogens (notably estrone and estradiol), converting them into their sulfated, inactive forms such as estrone sulfate. This modification increases water solubility and prevents estrogens from binding to estrogen receptors, thereby down-regulating their hormonal activity. SULT1E1 is mainly involved in the regulation of estrogen homeostasis but also acts on other substrates including dehydroepiandrosterone (DHEA) and several xenobiotics. Its expression is detected in multiple tissues including liver, breast, adipose tissue, endometrium, and brain, and is implicated in the pathophysiology of hormone-dependent cancers due to its regulatory control over estrogen availability. Certain drugs—including synthetic estrogens and tamoxifen metabolites—are also substrates for SULT1E1, and gene polymorphisms or altered expression levels have been associated with disease risk and variable drug responses.

Other names
Estrone sulfotransferaseSULT1E1ESTSulfotransferase 1E1Estrogen sulfotransferase 1
02

Mechanism of action

Sulfation (inactivation via sulfonation of estrogens and certain drugs, thereby regulating their bioavailability and interaction with estrogen receptors)

03

Biological functions

Estrogen inactivationHormone metabolismEstrogen homeostasisRegulation of estrogen receptor activitySulfation (phase II metabolism)Detoxification of endogenous and xenobiotic compounds
04

Disease associations

Cancer (notably hormone-dependent cancers, e.g., breast, endometrial, ovarian cancer)Endometrial cancerHormone-dependent diseaseInflammation (context-dependent)Type 2 diabetes (expression induced in tissue inflammation)
05

Safety considerations

Polymorphisms can reduce or alter enzymatic activity, possibly affecting drug response and disease susceptibilityAberrant expression may influence estrogen-dependent cancer risk
06

Interacting drugs

Fulvestrant

6 more in the full profile.

07

Biomarkers

Expression levels of SULT1E1/EST as prognostic markers in hormone-dependent cancers (e.g., endometrial, ovarian, breast cancer)Polymorphisms in SULT1E1 gene as risk modifiers in sex-hormone related cancers

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