Target intelligence / Profile preview

Prostanoid EP1 Receptor (EP1)

Target
EP1
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The Prostanoid EP1 receptor, also known as Prostaglandin E2 receptor 1 (EP1), is a G protein-coupled receptor (GPCR) that primarily binds prostaglandin E2 (PGE2). Activation leads to stimulation of phospholipase C (PLC), resulting in increased intracellular inositol trisphosphate (IP3) and diacylglycerol (DAG), which mobilizes intracellular calcium (Ca2+). It mediates various physiological functions, including smooth muscle contraction and has been implicated in neurodegenerative diseases and cancer. Antagonists have shown efficacy in preclinical models for reducing neurotoxicity.

Other names
Prostaglandin E2 Receptor 1PTGER1
02

Mechanism of action

Gq protein activation, phospholipase C (PLC) stimulation, increased intracellular inositol trisphosphate (IP3) and diacylglycerol (DAG), mobilization of intracellular calcium (Ca2+)

03

Biological functions

Signal transductionSmooth muscle contractionCalcium mobilizationNeurotransmission
04

Disease associations

Neurodegenerative diseasesAlzheimer's diseaseParkinson's diseaseStrokeAmyotrophic lateral sclerosisEpilepsyCancerNeurotoxicityNeuroinflammation
05

Safety considerations

Potential for neurotoxicity via increased calcium signalingSpecies-specific differences in tissue distribution
06

Interacting drugs

ONO-8713

3 more in the full profile.

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