Target intelligence / Profile preview

E-type Prostanoid Receptor 4 (EP4)

Target
EP4
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

EP4 is a G protein-coupled receptor for prostaglandin E2 (PGE2), a key lipid mediator involved in inflammation and various physiological processes. It is considered therapeutically promising due to its broad range of biological effects, including roles in inflammation, vascular function, thrombosis, cancer, and bone metabolism. Its diverse functions are context-dependent, with potential for both beneficial and detrimental effects.

Other names
Prostaglandin E2 receptor EP4Prostanoid EP4 receptorPGE2 receptor EP4 subtypePTGER4
02

Mechanism of action

Activation of Gs proteins leading to increased cAMP levels and subsequent activation of PKA, PI3K/AKT/mTOR, and ERK/MAPK pathways; inhibition of NF-kB activation.

03

Biological functions

Signal transductionInflammation modulationVascular tone regulationVasorelaxationAnti-thrombotic propertiesRegulation of cytokine productionBone metabolismGastric acid secretionLipid metabolismCell proliferationCell differentiationCell survivalAngiogenesis
04

Disease associations

InflammationCancerAsthmaMigrainePainTransplant rejectionNon-small-cell lung cancerThrombosis
05

Safety considerations

Tumor-promoting activities under certain conditionsContext-dependent functions

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