Target intelligence / Profile preview

Estradiol 17-beta-dehydrogenase 1 (17β-HSD1)

Target
17β-HSD1
Molecular classification
Enzyme, Oxidoreductase, Short-chain dehydrogenases/reductases (SDR)
01

Overview

Estradiol 17-beta-dehydrogenase 1 (17β-HSD1) is a key enzyme in steroid metabolism, primarily responsible for the interconversion of estrone (E1), a weak estrogen, and estradiol (E2), the most potent natural estrogen. It catalyzes the reversible reaction: estrone + NAD(P)H + H+ <=> estradiol-17β + NAD(P)+. It is highly expressed in ovarian tissue and overexpressed in certain cancers such as breast cancer. Targeted inhibition is considered a potential therapeutic strategy against hormone-dependent tumors.

Other names
HSD17B1EDH17B2EDHB17HSD17SDR28C1E2DH20-alpha-HSDEstradiol dehydrogenaseEstrogen 17(β)-oxidoreductaseHydroxysteroid (17-beta) dehydrogenase type I
02

Mechanism of action

Inhibition of Estradiol 17-beta-dehydrogenase 1, leading to reduced estradiol production.

03

Biological functions

Steroid metabolismEstrogen synthesisAndrogen synthesisRegulation of estrogen receptor activityDihydrotestosterone (DHT) inactivation
04

Disease associations

Breast cancerEndometrial cancerHormone-dependent tumors
05

Safety considerations

Potential for off-target effectsHormonal imbalances

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