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

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Book cover Targeting Trafficking in Drug Development

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 245))

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.

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Acknowledgments

The authors would like to acknowledge members of the Bräuner-Osborne lab and Dr. Maria Waldhoer for the helpful discussions. S.R.F. acknowledges funding from the Independent Research Fund Denmark | Medical Sciences, the Lundbeck Foundation, and the Augustinus Foundation.

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Authors and Affiliations

  1. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark

    Simon R. Foster & Hans Bräuner-Osborne

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  1. Simon R. Foster
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  2. Hans Bräuner-Osborne
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Correspondence to Hans Bräuner-Osborne .

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  1. Red de Apoyo a la Investigación, National Autonomous University of Mexico and Instituto Nacional de Ciencias, Médicas y Nutrición SZ, Mexico City, Mexico

    Alfredo Ulloa-Aguirre

  2. Dep of Anatomy, Physiology and Pharmacology, Auburn University, College of Veterinary Medicine, Auburn, Alabama, USA

    Ya-Xiong Tao

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Foster, S.R., Bräuner-Osborne, H. (2017). Investigating Internalization and Intracellular Trafficking of GPCRs: New Techniques and Real-Time Experimental Approaches. In: Ulloa-Aguirre, A., Tao, YX. (eds) Targeting Trafficking in Drug Development. Handbook of Experimental Pharmacology, vol 245. Springer, Cham. https://doi.org/10.1007/164_2017_57

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