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Posttranslational Regulation of G Protein-Coupled Receptors

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Methods for the Discovery and Characterization of G Protein-Coupled Receptors

Part of the book series: Neuromethods ((NM,volume 60))

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Abstract

The G protein-coupled receptors (GPCRs) are a superfamily of transmembrane receptors that ­structurally possess an extracellular amino terminus, seven transmembrane domains linked by extracellular and intracellular loops, and a cytoplasmic carboxyl terminus. They are synthesized by ribosomes and enter into the endoplasmic reticulum (ER), from which they are transported to Golgi apparatus and the trans-Golgi network (TGN) and finally move to the plasma membrane. At the plasma membrane, GPCRs receive environmental stimuli and relay the message to the cells. During these processes, GPCRs undergo posttranslational modifications that regulate their maturation, their function at the cell surface and even the ultimate fate of the internalized receptor after agonist treatment. There are four major types of posttranslational modifications – glycosylation, phosphorylation, palmitoylation, and ubiquitination, each of which has distinct roles in expression and function of GPCRs. In this ­chapter we discuss the methods to study these posttranslational modifications and the findings of posttranslational modifications and their functional consequences on GPCRs, using opioid receptors as the main examples. Moreover, the detailed steps of the main methods are depicted and also our thoughts on future directions of this avenue of research.

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Authors and Affiliations

  1. Department of Pharmacology, University of Minnesota Medical School, Minneapolis, MN, USA

    Yu Qiu

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  1. Yu Qiu
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  2. Ping-Yee Law
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Correspondence to Yu Qiu .

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  1. Center for Health Sciences, College of Osteopathic Medicine, Oklahoma State University, W. 17th Street 1111, Tulsa, 74107, Oklahoma, USA

    Craig W. Stevens

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Qiu, Y., Law, PY. (2011). Posttranslational Regulation of G Protein-Coupled Receptors. In: Stevens, C. (eds) Methods for the Discovery and Characterization of G Protein-Coupled Receptors. Neuromethods, vol 60. Humana Press. https://doi.org/10.1007/978-1-61779-179-6_7

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  • DOI: https://doi.org/10.1007/978-1-61779-179-6_7

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