In this review, we summarize the physiological roles of EP4, its molecular structure and intracellular signaling pathways, and how EP4 receptors might be targeted pharmacologically for the benefit of human disease, including vascular and …

An EP4 receptor is a type of cell surface receptor that, upon binding with PGE2, regulates cell signaling pathways, including cAMP/PKA-dependent pathways as well as other pathways like PI3K/AKT/mTOR and MAPK pathways.

2013年6月17日 · The EP4 prostanoid receptor is one of four receptor subtypes for prostaglandin E2. It belongs to the family of G protein-coupled receptors. It was originally identified, similar to the EP2 receptor as a G(s)α-coupled, adenylyl cyclase-stimulating receptor.

Prostaglandin E2 (PGE 2) receptor 4 (EP4) is one of four EP receptors commonly upregulated in the tumor microenvironment and plays vital roles in stimulating cell proliferation, invasion, and metastasis.

In this context, the EP4 receptor is currently emerging as most versatile and promising among PGE2 receptors. Anti-inflammatory, anti-thrombotic and vasoprotective effects have been proposed for the EP4 receptor, along with its recently described unfavorable tumor-promoting and pro-angiogenic roles.

Grapiprant is a targeted approach to pain management – it selectively blocks the EP4 receptor, does not interfere with the production of prostanoids, and therefore does not affect the other PG receptor pathways that are affected in animals treated with COX inhibitor NSAIDs.

2018年12月3日 · Prostaglandin E receptor EP4, a G-protein-coupled receptor, is involved in disorders such as cancer and autoimmune disease. Here, we report the crystal structure of human EP4 in complex...

EP 4 receptor agonist reduces MMP-2 and -9 activities and improves cardiac function in a rat model of ischemia-reperfusion injury.

The EP4 receptor is positively coupled to cAMP production. In forebrain, the EP4 receptor is expressed basally in neurons and at low levels in endothelial cells [66]. An expanding literature documents pro-survival effects of GPCRαs signaling, and of the EP4 receptor in particular, suggesting that the EP4 receptor, like its related EP2 receptor ...

2023年12月6日 · In this work, seeking to diversify EP4R antagonist scaffolds, we computationally dock over 400 million compounds against an EP4R crystal structure and experimentally validate 71 highly ranked,...