Target intelligence / Profile preview

Estradiol (specifically, 17β-estradiol) (E2)

Target
E2
Molecular classification
Estrogen, Steroid hormone, Organic compound (steroid lipid), Human metabolite
01

Overview

17β-Estradiol is a naturally occurring estrogen steroid hormone and the major female sex hormone in humans, vital for the development and maintenance of female reproductive tissues and secondary sexual characteristics. It exerts its physiological effects primarily by binding to estrogen receptors (ERα and ERβ), modulating gene expression and cellular signaling processes in multiple tissues. Estradiol is also involved in rapid nongenomic signal transduction and influences cardiovascular, bone, nervous, and immune systems. In medical practice, estradiol itself is used as a drug for hormone replacement, but as a molecule, it is not a "target" for drug action; rather, it is the ligand for target proteins (the estrogen receptors). Thus, references to "targeting" estradiol generally relate to either antagonizing its effects (through receptor blockade) or inhibiting its synthesis.

Other names
Estradiol-17ββ-estradiolE2oestradiol17β-oestradiol17-beta-estradiol
02

Mechanism of action

Estradiol binds to and activates estrogen receptors (ERα, ERβ), which are nuclear transcription factors, leading to gene regulation and cellular responses. It also acts via rapid, nongenomic pathways involving kinase signaling cascades.

03

Biological functions

Endogenous hormone regulating female reproductive and other physiologyRegulation of cell proliferationModulation of gene transcription (via nuclear estrogen receptors)Rapid nongenomic signaling (signal transduction)
04

Disease associations

Hormone-sensitive cancers (e.g. breast cancer, endometrial cancer)Cardiovascular diseaseOsteoporosisNeurodegenerative diseases (via hormonal pathways)Reproductive disorders
05

Safety considerations

Excess estradiol (endogenous or exogenous) is associated with increased risk of hormone-dependent cancers and thromboembolic eventsToxic effects can occur at high or pharmacological concentrations
06

Interacting drugs

Estradiol itself is the endogenous ligand; it is not a target but a ligand for estrogen receptors

2 more in the full profile.

07

Biomarkers

Estradiol levels (serum/plasma) as a biomarker for ovarian function, fertility, and monitoring certain cancers or endocrine disorders

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