Measuring β-Arrestin 2 Recruitment
G protein-coupled receptors (GPCRs) are a large family of transmembrane receptors that transmit signals from the outside to the inside of the cell through specific G-protein-dependent or -independent mechanisms. Ligand-induced β-arrestin recruitment plays a critical role in GPCR regulation through receptor desensitization and internalization and also mediates G-protein independent signal transduction. The kinetics of the GPCR/β-arrestin interaction varies for different GPCR receptors, affecting downstream signaling events.
NanoBiT® PPI technology can monitor ligand-induced β-arrestin recruitment in real time. By tagging the GPCR with one NanoBiT® subunit and β-arrestin with the other subunit, luminescence can be measured when the two proteins interact. These videos show an increase in luminescence following ligand-induced membrane recruitment of β-arrestin 2 for two different classes of GPCRs, demonstrating the difference in interaction kinetics.