G protein-coupled estrogen receptors

The G protein coupled estrogen receptor [GPER], also known as GPR30, is one of the multiple cellular receptors for estrogen, which also include the nuclear receptors ERα and ERβ.  The nuclear receptors are more associated with regulating gene expression, whereas GPER acts independently of ERα and ERβ and mediates rapid cellular signalling.  GPER is localized in the plasma membrane and is is widely distributed in neural, breast, placental, heart, ovarian, prostate, hepatic, vascular epithelial and lymphoid tissues.   Estrogen-regulated physiology can result in loss of reproductive function, cancer, cardiovascular and neurodegenerative disease, obesity, insulin resistance, endometriosis, and systemic lupus erythematosus.  GPER is a tumour suppressor in a wide range of cancer types and GPER activation promotes beneficial effects in several brain disorders.

Further reading

Prossnitz and Arterburn (2015) International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacol Rev. 67(3) 505 PMID: 26023144

Zimmerman et al (2016) GPER-novel membrane oestrogen receptor. Clin Sci (Lond).  30(12):1005 PMID: 27154744

Xu (2019) G Protein-Coupled Estrogen Receptor: A Potential Therapeutic Target in Cancer. Front Endocrinol. 10 725 PMID: 31708873

Rouhimoghadam et al (2020) Therapeutic Perspectives on the Modulation of G-Protein Coupled Estrogen Receptor, GPER, Function. Front Endocrinol. 11 591217 PMID: 33329395