Tchem GPER1 G-protein coupled estrogen receptor 1

Protein Summary

Description

G-protein coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. Stimulates cAMP production, calcium mobilization and tyrosine kinase Src inducing the release of heparin-bound epidermal growth factor (HB-EGF) and subsequent transactivation of the epidermal growth factor receptor (EGFR), activating downstream signaling pathways such as PI3K/Akt and ERK/MAPK. Mediates pleiotropic functions among others in the cardiovascular, endocrine, reproductive, immune and central nervous systems. Has a role in cardioprotection by reducing cardiac hypertrophy and perivascular fibrosis in a RAMP3-dependent manner. Regulates arterial blood pressure by stimulating vasodilation and reducing vascular smooth muscle and microvascular endothelial cell proliferation. Plays a role in blood glucose homeostasis contributing to the insulin secretion response by pancreatic beta cells. Triggers mitochondrial apoptosis during pachytene spermatocyte differentiation. Stimulates uterine epithelial cell proliferation. Enhances uterine contractility in response to oxytocin. Contributes to thymic atrophy by inducing apoptosis. Attenuates TNF-mediated endothelial expression of leukocyte adhesion molecules. Promotes neuritogenesis in developing hippocampal neurons. Plays a role in acute neuroprotection against NMDA-induced excitotoxic neuronal death. Increases firing activity and intracellular calcium oscillations in luteinizing hormone-releasing hormone (LHRH) neurons. Inhibits early osteoblast proliferation at growth plate during skeletal development. Inhibits mature adipocyte differentiation and lipid accumulation. Involved in the recruitment of beta-arrestin 2 ARRB2 at the plasma membrane in epithelial cells. Functions also as a receptor for aldosterone mediating rapid regulation of vascular contractibility through the PI3K/ERK signaling pathway. Involved in cancer progression regulation. Stimulates cancer-associated fibroblast (CAF) proliferation by a rapid genomic response through the EGFR/ERK transduction pathway. Associated with EGFR, may act as a transcription factor activating growth regulatory genes (c-fos, cyclin D1). Promotes integrin alpha-5/beta-1 and fibronectin (FN) matrix assembly in breast cancer cells. 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]

Uniprot Accession IDs

• Q99527
• A8K6C5
• B5BUJ1
• O00143
• O43494
• Q13631
• Q6FHL1
• Q96F42
• Q99981

Gene Name

• GPER1

Ensembl ID

• ENST00000297469
• ENSP00000297469
• ENSG00000164850
• ENST00000397088
• ENSP00000380277
• ENST00000397092
• ENSP00000380281
• ENST00000401670
• ENSP00000385151

Symbol

• CEPR
• CMKRL2
• DRY12
• GPER
• GPR30
• mER
• CEPR
• GPER
• DRY12
• FEG-1
• GPR30
• LERGU
• LyGPR
• CMKRL2
• LERGU2
• GPCR-Br

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
gene perturbation	0.99
cellular component	0.9
biological term	0.81
molecular function	0.76

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / G-protein Coupled Estrogen Receptor 1

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Estrogen (G Protein-coupled) Receptor / G-protein Coupled Estrogen Receptor 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1124   (req: < 5)

Gene RIFs: 264   (req: <= 3)

Antibodies: 394   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1124   (req: >= 5)

Gene RIFs: 264   (req: > 3)

Antibodies: 394   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 59

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 3

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 5