GPER1

Also known as 6330420K13Rik, CMKRL2, Ceprl, FEG-1, GPCR-Br, Gper, Gpr30

G protein-coupled estrogen receptor 1 (GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans is encoded by the GPER gene. GPER binds to and is activated by the female sex hormone estradiol and is responsible for some of the rapid effects that estradiol has on cells.

Gene data

GPER1

Name: G protein-coupled estrogen receptor 1
Type: protein-coding
Position: 1,082,208–1,094,511 (+)
Aliases: CEPR, CMKRL2, DRY12, FEG-1, GPCR-Br, GPER, GPR30, LERGU, LERGU2, LyGPR
Ensembl: ENSG00000164850
RefSeq RNA: NM_001031682.1, NM_001039966.2, NM_001098201.3, NM_001505.3
RefSeq protein: NP_001035055.1, NP_001091671.1, NP_001496.1

This gene encodes a multi-pass membrane protein that localizes to the endoplasmic reticulum and a member of the G-protein coupled receptor 1 family. This receptor binds estrogen and activates multiple downstream signaling pathways, leading to stimulation of adenylate cyclase and an increase in cyclic AMP levels, while also promoting 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. This receptor has been shown to play a role in diverse biological processes, including bone and nervous system development, metabolism, cognition, male fertility and uterine function. [provided by RefSeq, Aug 2017].

Gene Ontology

Article

17 sections

Contents

Discovery
Ligands
Agonists
Antagonists
Unknown
Non-ligand
Function
Role in cancer
Role in normal tissues
Reproductive tissue
Cardiovascular effects
Central nervous system activity
Metabolic roles
Role in neurological disorders
See also
References
External links

== Discovery == The classical estrogen receptors first characterized in 1958 are water-soluble proteins located in the interior of cells that are activated by estrogenenic hormones such as estradiol and several of its metabolites such as estrone or estriol. These proteins belong to the nuclear hormone receptor class of transcription factors that regulate gene transcription. Since it takes time for genes to be transcribed into RNA and translated into protein, the effects of estrogens binding to these classical estrogen receptors is delayed. However, estrogens are also known to have effects that are too fast to be caused by regulation of gene transcription. In 2005, it was discovered that a member of the G protein-coupled receptor (GPCR) family, GPR30 also binds with high affinity to estradiol and is responsible in part for the rapid non-genomic actions of estradiol. Based on its ability to bind estradiol, GPR30 was renamed as G protein-coupled estrogen receptor (GPER). GPER is localized in the plasma membrane but is predominantly detected in the endoplasmic reticulum.