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Target intelligence / Profile preview
G protein-coupled estrogen receptor 1 (GPER)
- Target
- GPER
- Molecular classification
- G protein-coupled receptor, GPCR superfamily, Seven-transmembrane domain receptor
01
Overview
G protein-coupled estrogen receptor 1 (GPER), also known as GPR30, is a seven-transmembrane domain G protein-coupled receptor that binds to and is activated by estradiol, mediating rapid non-genomic cellular responses. It is expressed widely and implicated in various physiological and pathological processes, including cancer, cardiovascular disease, metabolic disorders, and inflammation. GPER is a therapeutic target for estrogen-related diseases.
- Other names
- GPR30GPCR-Br
02
Mechanism of action
Modulates rapid, non-genomic cellular responses to estrogens distinct from classical nuclear estrogen receptors via intracellular signaling cascades including MAPK/ERK, PI3K, EGFR transactivation, HIF-induced pathway, IGF-R pathway, and NF-kB pathway.
03
Biological functions
Signal transductionCell proliferationImmune regulationReproductive developmentNervous system modulationEndocrine functionVascular tone regulationGlucose/lipid metabolism
04
Disease associations
CancerBreast cancerTesticular germ cell tumorsCardiovascular diseaseMetabolic disordersInflammation
05
Safety considerations
Potential for off-target effects due to broad tissue expressionComplex signaling pathways may lead to unpredictable consequencesContext-dependent effects may limit therapeutic efficacy
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