Target intelligence / Profile preview

Prostaglandin E receptor 2 (EP2) (EP2)

Target
EP2
Molecular classification
G protein-coupled receptor [1], Receptor [1], Prostanoid receptor [2]
01

Overview

The Prostaglandin E receptor 2 (EP2) is a G protein-coupled receptor (GPCR) that serves as one of the four primary receptors for prostaglandin E2 (PGE2) [1, 2]. Upon activation, EP2 primarily couples with the Gs protein, leading to the stimulation of adenylate cyclase and a subsequent increase in intracellular cyclic adenosine monophosphate (cAMP) levels [2]. This signaling pathway is critical for various physiological processes, including smooth muscle relaxation, vasodilation, and the modulation of immune and inflammatory responses [1, 3]. In the context of disease, EP2 is frequently overexpressed in several cancers, where it contributes to tumor progression and immune evasion by suppressing the activity of cytotoxic T cells and natural killer cells within the tumor microenvironment [3, 5]. Additionally, EP2 signaling is involved in the regulation of intraocular pressure, making it a target for glaucoma treatment [4]. Pharmacological intervention includes the use of EP2 agonists, such as omidenepag isopropyl, to treat ocular hypertension, while EP2 antagonists are being investigated as potential immunotherapeutic agents to enhance anti-tumor immunity [4, 5].

Other names
PTGER2Prostanoid EP2 receptorPGE2 receptor EP2 subtypePGE receptor EP2
02

Mechanism of action

EP2 agonists activate the Gs-adenylate cyclase-cAMP signaling pathway to induce physiological effects like vasodilation or intraocular pressure reduction, while EP2 antagonists block PGE2 binding to prevent immunosuppression and tumor growth [2, 3, 4].

03

Biological functions

Signal transduction [1]Immune response [3]Smooth muscle relaxation [1]Vasodilation [1]Ovulation [1]
04

Disease associations

Cancer [3]Inflammation [5]Glaucoma [4]Endometriosis [1]Neurodegenerative disease [1]
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Safety considerations

Systemic hypotension [4]Gastrointestinal irritation [1]Potential for promoting tumor growth with agonists [3]Impact on reproductive health [1]
06

Interacting drugs

Dinoprostone [1]

4 more in the full profile.

07

Biomarkers

PTGER2 mRNA expression [3]Intracellular cAMP levels [2]PGE2 concentration in tissue [3]

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