Structures of human prostaglandin F_2α receptor reveal the mechanism of ligand and G protein selectivity.

ABSTRACT: Prostaglandins and their receptors regulate various physiological processes. Carboprost, an analog of prostaglandin F_2α and an agonist for the prostaglandin F2-alpha receptor (FP receptor), is clinically used to treat postpartum hemorrhage (PPH). However, off-target activation of closely related receptors such as the prostaglandin E receptor subtype EP3 (EP3 receptor) by carboprost results in side effects and limits the clinical application. Meanwhile, the FP receptor selective agonist latanoprost is not suitable to treat PPH due to its poor solubility and fast clearance. Here, we present two cryo-EM structures of the FP receptor bound to carboprost and latanoprost-FA (the free acid form of latanoprost) at 2.7 Å and 3.2 Å resolution, respectively. The structures reveal the molec

SUBMITTER: Lv X 

PROVIDER: S-EPMC10709307 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature