Structural basis of peptide recognition and activation of endothelin receptors.

ABSTRACT: Endothelin system comprises three endogenous 21-amino-acid peptide ligands endothelin-1, -2, and -3 (ET-1/2/3), and two G protein-coupled receptor (GPCR) subtypes-endothelin receptor A (ET_AR) and B (ET_BR). Since ET-1, the first endothelin, was identified in 1988 as one of the most potent endothelial cell-derived vasoconstrictor peptides with long-lasting actions, the endothelin system has attracted extensive attention due to its critical role in vasoregulation and close relevance in cardiovascular-related diseases. Here we present three cryo-electron microscopy structures of ET_AR and ET_BR bound to ET-1 and ET_BR bound to the selective peptide IRL1620. These structures reveal a highly conserved recognition mode of ET-1 and characterize t

SUBMITTER: Ji Y 

PROVIDER: S-EPMC9992518 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature