Optimization of the prostaglandin F2α receptor for structural biology.

ABSTRACT: Prostaglandin F2ɑ (PGF2ɑ) is a bioactive lipid derived from arachidonic acid and is involved in many physiological and pathophysiological processes, such as parturition, vascular tone regulation, glaucoma and inflammation. It acts by binding to the Prostaglandin F2ɑ receptor (FP), a G Protein-Coupled Receptor (GPCR) that mediates signaling events by engaging intracellular heterotrimeric G protein effectors. The orthosteric binding site of lipid-binding receptors displays greater efficacy-dependent plasticity that hinders the design of ligands. Solving the structure of FP with ligands of different efficacies at an atomic level is important to fully understand its mechanism of activation and inhibition. Most purified FP-ligand complexes are unstable in vitro. The development of new X-ray cry

SUBMITTER: Salze M 

PROVIDER: S-EPMC12273924 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature