Prostaglandin E2 receptor 1, 2, and 4 (EP1, EP2, and EP4) (EP1, EP2, and EP4)

Prostaglandin E2 receptors EP1, EP2, and EP4 are G protein-coupled receptors that mediate the diverse physiological and pathological effects of prostaglandin E2 (PGE2) (nih.gov, wikipedia.org). EP1 is primarily coupled to Gq proteins, leading to increased intracellular calcium levels, while EP2 and EP4 are coupled to Gs proteins, which stimulate the production of cyclic AMP (cAMP) (nih.gov). These receptors are involved in a wide range of biological processes, including the regulation of vascular tone, pain transmission, and inflammatory responses (nih.gov, researchgate.net). In the context of oncology, EP2 and EP4 are particularly significant as they are often overexpressed in the tumor microenvironment, where they promote immune evasion by suppressing the activity of cytotoxic T cells and natural killer cells while enhancing the suppressive function of regulatory T cells (frontiersin.org, pnas.org). Consequently, these receptors have become prominent therapeutic targets, with dual EP2/EP4 antagonists currently in clinical development to enhance the efficacy of cancer immunotherapies (nih.gov). Additionally, selective modulation of these receptors is being explored for the treatment of chronic pain, inflammatory bowel disease, and bone-related disorders (nih.gov).

Other names

PTGER1PTGER2PTGER4Prostanoid EP1 receptorProstanoid EP2 receptorProstanoid EP4 receptorPGE receptor 1PGE receptor 2PGE receptor 4PGE2 receptor 1PGE2 receptor 2PGE2 receptor 4

Antagonism of EP2 and EP4 receptors to inhibit PGE2-mediated immunosuppression and tumor progression; antagonism of EP1 for pain and inflammation; selective agonism for tissue repair and bone formation (nih.gov, frontiersin.org).