Understanding the molecular mechanism of endothelin ET_A receptor selecting isopeptides endothelin-1 and -3.

ABSTRACT: Endothelin-1 and -3 (ET1 and ET3) are potent vasoconstricting isopeptides that are involved in the pathophysiology of various diseases, such as cardiovascular and renal diseases. The two ETs exert their effects by binding to two G-protein-coupled receptors (GPCRs), the endothelin ET_A receptor (ET_AR) and the endothelin ET_B receptor (ET_BR). ET_AR and ET_BR reveal different preferences in the recognition of the two ETs: The binding affinity of ET_AR with ET1 is much higher than that with ET3, while the binding affinities of ET_BR with the two ETs are similar. Recently, the structures of ET_BR with ET1 and ET3 were determined. These crystal structures provide detailed descriptions of how ET_B

SUBMITTER: Wang L 

PROVIDER: S-EPMC9300638 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature