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Target intelligence / Profile preview
Prostaglandin E EP3 Receptor (EP3 receptor)
- Target
- EP3 receptor
- Molecular classification
- G protein-coupled receptor, GPCR, Rhodopsin-like GPCR, Subfamily A14
01
Overview
The Prostaglandin E EP3 receptor (EP3 receptor) is a G protein-coupled receptor (GPCR) that binds prostaglandin E2 (PGE2), a bioactive lipid involved in numerous physiological and pathological processes. The human gene encoding this receptor is PTGER3, located on chromosome 1p31.1. Humans express at least eight isoforms of the EP3 receptor due to alternative splicing, resulting in proteins with variable C-terminal regions and diverse signaling pathways. EP3 receptor activation mediates various functions including pain modulation, negative regulation of glucose-stimulated insulin secretion, vasoconstriction, and platelet aggregation. Its role varies across diseases, with both pro-tumorigenic and anti-tumorigenic roles described in cancer.
- Other names
- PTGER3
02
Mechanism of action
Gi-coupled inhibition of adenylate cyclase, Gq-coupled increase in intracellular calcium, Gs-coupled increase in cAMP (isoform-dependent)
03
Biological functions
Signal transductionPain modulationAnalgesiaMetabolic regulationRegulation of insulin secretionVasoconstrictionPlatelet aggregationFever response
04
Disease associations
InflammationPainDiabetesVascular diseasesCancer
05
Safety considerations
Potential for complex and context-dependent effects due to multiple splice variantsPro-tumorigenic and anti-tumorigenic roles described in cancer biology, requiring careful consideration of expression levels and disease context
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