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Prostaglandin E2 Receptor 2 (EP2)
- Target
- EP2
- Molecular classification
- G protein-coupled receptor, GPCR, Rhodopsin-like GPCR, Subfamily A14
01
Overview
Prostaglandin E2 receptor 2 (EP2) is a G protein-coupled receptor (GPCR) that binds prostaglandin E2 (PGE₂), a key lipid mediator derived from arachidonic acid. It primarily couples to Gαs proteins, leading to increased intracellular cAMP and activation of PKA/Epac. EP2 mediates diverse physiological effects, including smooth muscle relaxation and modulation of immune responses. It has been implicated in several disease processes, including cancer, neurological disorders, and pulmonary fibrosis, making it a potential therapeutic target.
- Other names
- Prostaglandin E₂ Receptor 2PTGER2
02
Mechanism of action
Agonism of EP2 leads to Gαs protein activation, increasing cAMP production and downstream signaling via PKA/Epac. Antagonism inhibits PGE2-mediated EP2 signaling.
03
Biological functions
Smooth muscle relaxationImmune modulationSignal transductionRegulation of gastrointestinal functionscAMP productionPKA activationEpac activation
04
Disease associations
CancerInflammationNeurodegenerative diseasePulmonary fibrosisIBDColorectal neoplasia
05
Safety considerations
Potential for both pro- and anti-inflammatory effects depending on contextTargeting EP2 in cancer requires careful consideration due to its complex role in tumor developmentPotential side effects associated with modulating cAMP levels
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