Discovery of β-arrestin-biased β₂-adrenoceptor agonists from 2-amino-2-phenylethanol derivatives.

ABSTRACT: β-Arrestins are a small family of proteins important for signal transduction at G protein-coupled receptors (GPCRs). β-Arrestins are involved in the desensitization of GPCRs. Recently, biased ligands possessing different efficacies in activating the G protein- versus the β-arrestin-dependent signals downstream of a single GPCR have emerged, which can be used to selectively modulate GPCR signal transduction in such a way that desirable signals are enhanced to produce therapeutic effects while undesirable signals of the same GPCR are suppressed to avoid side effects. In the present study, we evaluated agonist bias for compounds developed along a drug discovery project of β₂-adrenoceptor agonists. About 150 compounds, including derivatives of fenoterol, 2-amino-1-phenylethanol and

SUBMITTER: Woo AY 

PROVIDER: S-EPMC6786399 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature