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Target intelligence / Profile preview
Prostaglandin E EP4 Receptor (PTGER4)
- Target
- PTGER4
- Molecular classification
- G protein-coupled receptor, GPCR, Prostanoid receptor, Receptor
01
Overview
The Prostaglandin E EP4 receptor (PTGER4) is a G protein-coupled receptor that binds prostaglandin E2 (PGE2), mediating smooth muscle relaxation and playing diverse roles in inflammation, immunity, and vascular biology. It is implicated in various diseases, including asthma, migraine, pain, transplant rejection, and cancer. Selective agonists and antagonists are being explored for therapeutic potential.
- Other names
- Prostanoid EP4 receptorPGE2 receptor EP4 subtype
02
Mechanism of action
Activation of Gαs protein, stimulation of adenylate cyclase, increase in intracellular cAMP, activation of protein kinase A (PKA), phosphorylation of CREB, activation of PI3K/AKT/mTOR and MAPKs such as ERK and p38
03
Biological functions
Smooth muscle relaxationRegulation of renal hemodynamicsIntestinal epithelial transportAdrenal aldosterone secretion regulationImmune suppressionVascular neointimal hyperplasiaSignal transductionCell proliferationCell differentiationCell survivalAngiogenesis
04
Disease associations
AsthmaMigrainePainTransplanted organ/tissue rejectionNon-small-cell lung cancerInflammationCancerCardiovascular disease
05
Safety considerations
Potential tumor-promoting actions due to proangiogenic propertiesContext-dependent effects (anti-inflammatory vs. pro-tumorigenic)
06
Interacting drugs
PGE2
1 more in the full profile.
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