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Target intelligence / Profile preview
G protein-coupled estrogen receptor (GPER)
- Target
- GPER
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
G protein-coupled estrogen receptor (GPER), also known as GPR30 or GPER1, is a seven-transmembrane domain receptor and member of the GPCR family. It binds with high affinity to 17β-estradiol (E2) and mediates rapid non-genomic signaling events, activating pathways like cAMP/PKA, PLC/IP₃/Ca²⁺, PI3K/Akt, and MAPKs. GPER is expressed in various tissues, playing roles in cardiovascular regulation, immune modulation, and metabolic regulation. It is implicated in diseases such as cancer, cardiovascular disorders, and metabolic disorders, making it a therapeutic target for selective agonists/antagonists.
- Other names
- GPR30GPER1
02
Mechanism of action
Agonists and antagonists modulate GPER activity, impacting downstream signaling pathways such as cAMP/PKA, PLC/IP₃/Ca²⁺, PI3K/Akt, and MAPKs. This leads to rapid non-genomic effects and modulation of gene expression.
03
Biological functions
Signal transductionCardiovascular regulationImmune modulationMetabolic regulationCell proliferationCell survival
04
Disease associations
CancerCardiovascular diseaseMetabolic disordersAutoimmune diseasesInflammation
05
Safety considerations
Potential for off-target effects if GPER targeting is not selective.Unclear long-term effects of chronic GPER modulation.
06
Interacting drugs
17β-estradiol (E2)
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