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Target intelligence / Profile preview
Prostanoid EP4 Receptor (EP4)
- Target
- EP4
- Molecular classification
- G protein-coupled receptor, GPCR, Prostanoid receptor
01
Overview
The EP4 receptor is a prostaglandin receptor subtype that binds PGE2. It is a GPCR that primarily couples to Gs, leading to increased cAMP levels and downstream signaling events. It plays diverse roles in vasodilation, inflammation, bone remodeling, and other physiological processes. Therapeutic targeting of EP4 is of interest for various diseases including asthma, cancer, and inflammatory conditions.
- Other names
- Prostaglandin E2 receptor EP4 subtypePGE2 receptor EP4 subtypePTGER2
02
Mechanism of action
Activation of Gs proteins, leading to increased cAMP levels and PKA activation. Can also couple with Gi proteins, β-arrestin, and activate PI3K/AKT/mTOR, ERK/MAPK, and p38 MAPK pathways.
03
Biological functions
Signal transductionVasodilationInflammation modulationBone remodelingCytoprotectionAngiogenesisPain perception modulation
04
Disease associations
AsthmaMigrainePain syndromesTransplant rejection/inflammation controlNon-small-cell lung cancerRheumatoid arthritisColitisHypertensionCancer
05
Interacting drugs
L-902688
4 more in the full profile.
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