Investigating internalization and intracellular trafficking of GPCRs: New techniques and real-time experimental approaches

Simon R. Foster, Hans Bräuner-Osborne

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Otherpeer-review

26 Citations (Scopus)


The ability to regulate the interaction between cells and their extracellular environment is essential for the maintenance of appropriate physiological function. For G protein-coupled receptors (GPCRs), this regulation occurs through multiple mechanisms that provide spatial and temporal control for signal transduction. One of the major mechanisms for GPCR regulation involves their endocytic trafficking, which serves to internalize the receptors from the plasma membrane and thereby attenuate G protein-dependent signaling. However, there is accumulating evidence to suggest that GPCRs can signal independently of G proteins, as well as from intracellular compartments including endosomes. It is in this context that receptor internalization and intracellular trafficking have attracted renewed interest within the GPCR field. In this chapter, we will review the current understanding and methodologies that have been used to investigate internalization and intracellular signaling of GPCRs, with a particular focus on emerging real-time techniques. These recent developments have improved our understanding of the complexities of GPCR internalization and intracellular signaling and suggest that the broader biological relevance and potential therapeutic implications of these processes remain to be explored.

Original languageEnglish
Title of host publicationTargeting Trafficking in Drug Development
EditorsAlfredo Ulloa-Aguirre, Ya-Xiong Tao
Number of pages21
ISBN (Electronic)9783319741642
ISBN (Print)9783319741635
Publication statusPublished - 1 Jan 2018
Externally publishedYes

Publication series

NameHandbook of Experimental Pharmacology
ISSN (Print)0171-2004
ISSN (Electronic)1865-0325


  • Arrestin
  • Endosome
  • G protein-coupled receptor
  • Internalization
  • Signaling
  • SNAP-tag

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