A novel luminescence-based β-arrestin recruitment assay for unmodified receptors.

ABSTRACT: G protein-coupled receptors (GPCRs) signal through activation of G proteins and subsequent modulation of downstream effectors. More recently, signaling mediated by β-arrestin has also been implicated in important physiological functions. This has led to great interest in the identification of biased ligands that favor either G protein or β-arrestin-signaling pathways. However, nearly all screening techniques for measuring β-arrestin recruitment have required C-terminal receptor modifications that can in principle alter protein interactions and thus signaling. Here, we have developed a novel luminescence-based assay to measure β-arrestin recruitment to the membrane or early endosomes by unmodified receptors. Our strategy uses NanoLuc, an engineered luciferase from Oplophorus gracilirostris

SUBMITTER: Hauge Pedersen M 

PROVIDER: S-EPMC8027564 | biostudies-literature | 2021 Jan-Jun

REPOSITORIES: biostudies-literature