GPR30

GPR30

G protein-coupled estrogen receptor 1
Identifiers
GPER Gene
RNA expression pattern

G protein-coupled estrogen receptor 1 (GPER) also known as the G protein-coupled receptor 30 (GPR30) is a G protein-coupled receptor that in humans is encoded by the GPER gene.[1] GPR30 is an integral membrane protein with high affinity for estrogen.[2][3][4][5]

Function

This protein is a member of the rhodopsin-like family of G protein-coupled receptors and is a multi-pass membrane protein that localizes to the endoplasmic reticulum. The protein binds estrogen, resulting in intracellular calcium mobilization and synthesis of phosphatidylinositol (3,4,5)-trisphosphate in the nucleus. This protein therefore plays a role in the rapid nongenomic signaling events widely observed following stimulation of cells and tissues with estrogen. Alternate transcriptional splice variants that encode the same protein have been characterized.[6] The distribution of GPR30 is well established in the rodent, with high expression observed in the hypothalamus, pituitary gland, adrenal medulla, kidney medulla and developing follicles of the ovary.[7]

Animal studies

Female GPR30 knockout mice display hyperglycemia and impaired glucose tolerance, reduced body growth, and increased blood pressure.[8] Male GPR30 knockout mice are observed to have increased growth, body fat, increased osteoblast function (mineralization) resulting in higher bone mineral density and trabecular bone volume, and persistent growth plate activity resulting in longer bones.[9]

Clinical significance

GPR30 plays an important role in development of tamoxifen resistance in breast cancer cells.[10]

References

Further reading

External links

  • Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.