15-Keto-PGE₂ acts as a biased/partial agonist to terminate PGE₂-evoked signaling.

ABSTRACT: Prostaglandin E₂ (PGE₂) is well-known as an endogenous proinflammatory prostanoid synthesized from arachidonic acid by the activation of cyclooxygenase-2. E type prostanoid (EP) receptors are cognates for PGE₂ that have four main subtypes: EP1 to EP4. Of these, the EP2 and EP4 prostanoid receptors have been shown to couple to Gα_s-protein and can activate adenylyl cyclase to form cAMP. Studies suggest that EP4 receptors are involved in colorectal homeostasis and cancer development, but further work is needed to identify the roles of EP2 receptors in these functions. After sufficient inflammation has been evoked by PGE₂, it is metabolized to 15-keto-PGE₂ Thus, 15-keto-PGE₂ has long been considered an inactive metabo

SUBMITTER: Endo S 

PROVIDER: S-EPMC7504929 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature