Estrogen and Related Receptor Agonists Small Molecules and Peptides

The GPER (G protein-coupled estrogen receptor, GPR30) is a membrane protein that binds estrogen leading to estrogen-mediated adenylyl cyclase stimulation. The receptor is widely distributed in neural, breast, placental, heart, ovarian, prostate, hepatic, vascular epithelial and lymphoid tissues. The GPER binds estradiol with high affinity, but has lower affinity for the other estrogens, estrone and estriol. The receptor acts independently of ERα and ERβ and triggers ER-dependent EGFR action.