Estrogen Receptors (ERα, ERβ, GPER) (ERα, ERβ, GPER)

Estrogen receptors comprise two classic nuclear hormone receptors (estrogen receptor alpha and estrogen receptor beta) and a membrane-bound G protein-coupled receptor (GPER, formerly GPR30). ERα and ERβ function primarily as ligand-activated transcription factors, regulating gene expression upon binding estrogens such as 17β-estradiol, and are central to the maintenance, development, and physiology of reproductive and other tissues. GPER mediates rapid, non-genomic signaling events of estrogens as a seven-transmembrane GPCR. All three receptors contribute to various physiological and pathological roles, most notably in cancer, cardiovascular disease, immune regulation, and reproductive system disorders. These receptors are established therapeutic targets for selective modulators and antagonists, which are widely used in endocrine therapy, especially for hormone-sensitive cancers like breast cancer, and are the focus of ongoing drug discovery efforts[4][5][1][2][6]. If you require a single standardized entry, these should be split by their molecular identity (ERα, ERβ, GPER) in structured databases.

Other names

ESR1NR3A1nuclear estrogen receptor alphaESR2NR3A2nuclear estrogen receptor betaGPR30

Modulation of estrogen-responsive gene transcription (ERα, ERβ). Activation or inhibition of non-genomic estrogen signaling pathways (GPER). Induction of apoptosis or inhibition of proliferation in hormone-dependent tumors. Selective modulation or inhibition of estrogen action depending on tissue, ligand, and target.