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Physiological Role of G-Protein Coupled Receptor Phosphorylation

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Muscarinic Receptors

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 208))

Abstract

It is now well established that G-protein coupled receptors (GPCRs) are hyper-phosphorylated following agonist occupation usually at serine and threonine residues contained on the third intracellular loop and C-terminal tail. After some 2 decades of intensive research, the nature of protein kinases involved in this process together with the signalling consequences of receptor phosphorylation has been firmly established. The major challenge that the field currently faces is placing all this information within a physiological context and determining to what extent does phosphoregulation of GPCRs impact on whole animal responses. In this chapter, we address this issue by describing how GPCR phosphorylation might vary depending on the cell type in which the receptor is expressed and how this might be employed to drive selective regulation of physiological responses.

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Abbreviations

GPCR:

G-protein coupled receptor

GRK:

G-protein coupled receptor kinase

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Authors and Affiliations

  1. Department of Cell Physiology and Pharmacology, University of Leicester, Hodgkin Building, Lancaster Road, Leicester, LE1 9HN, UK

    Adrian J. Butcher, Kok Choi Kong & Andrew B. Tobin

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  1. Adrian J. Butcher
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  2. Kok Choi Kong
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  3. Rudi Prihandoko
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  4. Andrew B. Tobin
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Correspondence to Andrew B. Tobin .

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Editors and Affiliations

  1. UHN67, Department of Pulmonary and Critical Ca, Oregon Health & Science University, SW Sam Jackson Park Road 3181, Portland, 97239, Oregon, USA

    Allison D. Fryer

  2. , Department of Pharmacology, Monash Institute of Pharmaceutical Scien, Royal Parade 381, Parkville, 3052, Victoria, Australia

    Arthur Christopoulos

  3. , Department of Pharmacology, University of Washington, Seattle, 98195-7750, Washington, USA

    Neil M. Nathanson

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Butcher, A.J., Kong, K.C., Prihandoko, R., Tobin, A.B. (2012). Physiological Role of G-Protein Coupled Receptor Phosphorylation. In: Fryer, A., Christopoulos, A., Nathanson, N. (eds) Muscarinic Receptors. Handbook of Experimental Pharmacology, vol 208. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-23274-9_5

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