Structural insights into the peptide selectivity and activation of human neuromedin U receptors.

ABSTRACT: Neuromedin U receptors (NMURs), including NMUR1 and NMUR2, are a group of G_q/11-coupled G protein-coupled receptors (GPCRs). NMUR1 and NMUR2 play distinct, pleiotropic physiological functions in peripheral tissues and in the central nervous system (CNS), respectively, according to their distinct tissue distributions. These receptors are stimulated by two endogenous neuropeptides, neuromedin U and S (NMU and NMS) with similar binding affinities. NMURs have gathered attention as potential drug targets for obesity and inflammatory disorders. Specifically, selective agonists for NMUR2 in peripheral tissue show promising long-term anti-obesity effects with fewer CNS-related side effects. However, the mechanisms of peptide binding specificity and receptor activation remain elusive. He

SUBMITTER: You C 

PROVIDER: S-EPMC9019041 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature