Investigation of adenosine A1 receptor-mediated β-arrestin 2 recruitment using a split-luciferase assay.

ABSTRACT: Background: Adenosine A1 receptor (A₁AR) plays a prominent role in neurological and cardiac diseases and inflammatory processes. Its endogenous ligand adenosine is known to be one of the key players in the sleep-wake cycle. Like other G protein-coupled receptors (GPCRs), stimulation of A₁AR leads to the recruitment of arrestins in addition to the activation of G proteins. So far, little is known about the role of these proteins in signal transduction and regulation of A₁AR compared to the activation of G proteins. In this work, we characterized a live cell assay for A₁AR-mediated β-arrestin 2 recruitment. We have applied this assay to a set of different compounds that interact with this receptor. Methods: Based on NanoBit^®

SUBMITTER: Saecker L 

PROVIDER: S-EPMC10268005 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature