G protein-coupled estrogen receptor

G protein-coupled estrogen receptor (GPER), also known as GPR30, is a protein that in humans is encoded by the GPER gene. GPER is a member of the G protein-coupled receptor family of proteins, which play a crucial role in cellular signaling and function.

Function

GPER is a seven-transmembrane domain receptor that is activated by the hormone estrogen. Upon activation, GPER can initiate a variety of intracellular signaling pathways, including the phosphatidylinositol 3-kinase (PI3K) pathway and the mitogen-activated protein kinase (MAPK) pathway. These signaling pathways are involved in a variety of cellular processes, including cell growth, differentiation, and survival.

Clinical significance

GPER has been implicated in a number of diseases, including breast cancer, ovarian cancer, and endometrial cancer. In these diseases, overexpression of GPER has been associated with a poor prognosis. GPER is also involved in the regulation of blood pressure and cardiovascular disease, and has been implicated in the pathogenesis of obesity and diabetes.

Therapeutic potential

Because of its role in disease, GPER is a potential target for therapeutic intervention. Several GPER agonists and antagonists have been developed and are currently being tested in preclinical and clinical trials. These compounds have the potential to modulate the activity of GPER and thereby alter the course of diseases in which GPER is involved.

See also

• Estrogen receptor
• G protein-coupled receptor
• Breast cancer
• Ovarian cancer
• Endometrial cancer

References

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