Prostaglandin E receptor (EP receptor) (EP receptor)

Prostaglandin E receptors (EP receptors) are a family of four distinct G protein-coupled receptors, designated EP1, EP2, EP3, and EP4, that mediate the diverse biological effects of Prostaglandin E2 (PGE2) (IUPHAR/BPS Guide to Pharmacology, 2023). These receptors are widely distributed throughout the body and are essential for regulating physiological processes such as inflammation, pain perception, gastric acid secretion, and vascular tone (UniProt, 2024). Each subtype is coupled to different intracellular signaling pathways: EP1 typically signals through Gq to increase calcium; EP2 and EP4 signal through Gs to increase cAMP; and EP3 primarily signals through Gi to decrease cAMP (PubMed, PMID: 28463611). In clinical medicine, EP receptors are significant therapeutic targets; for example, EP3 and EP4 agonists are used for gastroprotection and labor induction, while EP2 agonists are used to treat glaucoma (StatPearls, 2023). Furthermore, the EP4 receptor has emerged as a key target in oncology, as its signaling in the tumor microenvironment promotes immune evasion and cancer progression (Nature Reviews Drug Discovery, 2017). Consequently, both selective agonists and antagonists are actively utilized or under development to address a broad spectrum of inflammatory, cardiovascular, and malignant diseases.

Other names

PGE2 receptorProstanoid EP receptorPTGEREP1EP2EP3EP4

EP receptors modulate intracellular signaling by coupling with various G-proteins (Gs, Gi, or Gq) upon binding Prostaglandin E2. Agonists are utilized to stimulate physiological responses like cervical ripening or gastric protection, whereas antagonists are designed to inhibit PGE2-driven inflammation, pain, and tumor-mediated immunosuppression (IUPHAR/BPS Guide to Pharmacology, 2023; PubMed, PMID: 30107145).