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GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity pp 67–81Cite as

The Functional Size of GPCRs – Monomers, Dimers or Tetramers?

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Part of the book series: Subcellular Biochemistry ((SCBI,volume 63))

Abstract

In almost 16 years since the word “dimer” was used in a publication to describe the organization of G protein-coupled receptors (GPCRs), a large number of studies have since weighed in on this notion. Are native, functional GPCRs monomers, dimers or as some would suggest even higher order structures? Here, we review some of the latest evidence regarding the organization of these receptors in both homo- and hetero-oligomeric formats, with a particular focus on β-adrenergic receptors. This is particularly important for understanding the allosteric nature of receptor/receptor interactions. It is likely that, over the course of evolution, mechanisms have come into play using all of the possible variations in receptor/receptor stoichiometry, depending on the cell and the physiological context in question. Finally, we provide some data that suggests that higher order structures of GPCRs, as with dimers themselves are probably assembled in the ER.

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Acknowledgments

This work was supported by grants from the Canadian Institutes of Health Research to T.E.H (MOP-36379) as well as the CIHR Team in GPCR Allosteric Regulation (CTiGAR). T.E.H. is a Chercheur National of the Fonds de la Recherche en Santé du Québec (FRSQ). We thank Vic Rebois (NIH) and the Hébert lab for helpful discussions.

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  1. Department of Pharmacology and Therapeutics, McGill University, Room 1303 McIntyre Medical Sciences Building, 3655 Promenade Sir William Osler, Montréal, QC, H3G 1Y6, Canada

    Darlaine Pétrin & Terence E. Hébert

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  1. Darlaine Pétrin
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  2. Terence E. Hébert
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Correspondence to Terence E. Hébert .

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Editors and Affiliations

  1. Faculty of Medicine, Pharmacology, Dalhousie University, College Street 5968, Halifax, B3H 4R2, Nova Scotia, Canada

    Denis J. Dupré

  2. , Pharmacology and Therapeutics, McGill University, Promenade Sir William Osler 3655, Montreal, H3G 1Y6, Québec, Canada

    Terence E. Hébert

  3. Institut Cochin, Rue Méchain 22, Paris, 75014, France

    Ralf Jockers

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Pétrin, D., Hébert, T.E. (2012). The Functional Size of GPCRs – Monomers, Dimers or Tetramers?. In: Dupré, D., Hébert, T., Jockers, R. (eds) GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity. Subcellular Biochemistry, vol 63. Springer, Dordrecht. https://doi.org/10.1007/978-94-007-4765-4_4

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