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Target intelligence / Profile preview
Prostaglandin E receptor 4 (EP4)
- Target
- EP4
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
Prostaglandin E receptor 4 (EP4) is a G protein-coupled receptor that binds prostaglandin E2 (PGE2). Upon activation, it primarily couples to Gs proteins, leading to increased intracellular cAMP levels. EP4 is widely expressed on immune cells and plays a role in various physiological and pathological processes, including smooth muscle relaxation, immune modulation, and cancer progression. It is a significant target for anti-inflammatory and immuno-oncology therapies.
- Other names
- PTGER4Prostanoid EP4 receptorProstaglandin E2 receptor EP4 subtypePGE2 receptor EP4 subtype
02
Mechanism of action
Agonism of EP4 receptor increases cAMP and activates protein kinase A (PKA), which in turn activates transcription factors such as CREB. Antagonism of EP4 can restore anti-tumor immunity by reactivating NK cell functions and restoring recruitment/functionality of cross-presenting DCs within tumors.
03
Biological functions
Signal transductionSmooth muscle relaxationImmune response regulationCell proliferationCell differentiationCell survivalAngiogenesis
04
Disease associations
AsthmaMigrainePainTransplant rejection/modulationNon-small-cell lung cancerColorectal cancerCancerInflammation
05
Safety considerations
ImmunosuppressionPotential for off-target effects due to widespread expression
06
Interacting drugs
ONO-AE3‑208
2 more in the full profile.
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