Investigating Internalization and Intracellular Trafficking of GPCRs: New Techniques and Real-Time Experimental Approaches

Simon R Foster, Hans Bräuner-Osborne

    82 Citations (Scopus)

    Abstract

    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 publicationHandbook of Experimental Pharmacology
    Volume245
    PublisherSpringer
    Publication date11 Oct 2017
    Pages41-61
    DOIs
    Publication statusPublished - 11 Oct 2017
    SeriesHandbook of Experimental Pharmacology
    ISSN0171-2004

    Keywords

    • Journal Article

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