Single-Molecule Imaging of GPCR Interactions

Davide Calebiro, Titiwat Sungkaworn

Research output: Contribution to journalReview articlepeer-review

37 Citations (Scopus)


G protein-coupled receptors (GPCRs) constitute the largest family of membrane receptors and are of great interest as pharmacological targets. Although the occurrence of GPCR signaling nanodomains has long been hypothesized based on indirect evidence, this and other fundamental aspects of GPCR signaling have been difficult to prove. The advent of single-molecule microscopy methods, which allow direct visualization of individual membrane proteins with unprecedented spatiotemporal resolution, provides unique opportunities to address several of these open questions. Indeed, recent single-molecule studies have revealed that GPCRs and G proteins transiently interact with each other as well as with structural components of the plasma membrane, leading to the formation of dynamic complexes and ‘hot spots’ for GPCR signaling. Whereas we are only beginning to understand the implications of this unexpected level of complexity, single-molecule approaches are likely to play a crucial role to further dissect the protein–protein interactions that are at the heart of GPCR signaling.
Original languageEnglish
Pages (from-to)109-122
JournalTrends in Pharmacological Sciences
Issue number2
Early online date17 Nov 2017
Publication statusE-pub ahead of print - 17 Nov 2017


  • dimerization
  • GPCR
  • labeling
  • nanodomains
  • single-molecule microscopy


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