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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 mitoch ...more
Uniprot Accession IDs
Gene Name
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
Illumination Graph
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


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: 248   (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: 248   (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