Optical approaches for visualization of arrestin binding to muscarinic receptor.

G protein-coupled seven-transmembrane receptors (GPCRs) mediate responses to hormones, metabolites, lipids, and neurotransmitters at the cell membrane, and so they are prominent drug targets. Although many structural, biochemical, cell biological, and biophysical studies made remarkable progress to understand mechanisms of GPCR signaling, there still are many unanswered questions about arrestin-dependent GPCR signaling. In this chapter, we focus on optical assays to see muscarinic receptor-arrestin interactions with ensemble FRET and single-molecule TIRF imaging in live cells and finally to integrate the information to simulate hypothesized steps in Virtual Cell.