G protein- and β-arrestin Signaling Profiles of Endothelin Derivatives at the Type A Endothelin Receptor.

ABSTRACT:

Background

Endothelin-1 (ET-1) is a potent vasoconstrictor in the cardiovascular system, an effect mediated through the type A endothelin receptor (ET_AR), a G protein-coupled receptor (GPCR). Antagonists of the ET_AR have shown promising results in randomized clinical trials. However, side effects limit widespread use. Biased agonists have been developed to mitigate the untoward effects of a number of GPCR antagonists. These agents block deleterious G-coupled pathways while stimulating protective β-arrestin pathways. The goal of this study was to test whether there was any significant ligand bias between endothelin derivatives, and whether this could have any physiologic effects in the cardiovascular system.

Methods

A panel of endothelin derivativ

SUBMITTER: Xiong X 

PROVIDER: S-EPMC8786096 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature