RESEARCH ARTICLE


On the Role of G Protein-Coupled Receptors Oligomerization



Maricel Gómez-Soler, Siobhán Ahern, Víctor Fernández-Dueñas, Francisco Ciruela*
University of Barcelona, Unitat de Farmacologia, Dept. de Patologia i Terapeutica Experimental, Facultat de Medicina (Campus de Bellvitge), Pavelló de Govern, Av. Feixa Llarga, s/n, 08907 L'Hospitalet del Llobregat, Barcelona, Spain.


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© 2010 Gómez-Soler et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: https://creativecommons.org/licenses/by/4.0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the University of Barcelona, Unitat de Farmacologia, Dept. de Patologia i Terapeutica Experimental, Facultat de Medicina (Campus de Bellvitge), Pavelló de Govern, Av. Feixa Llarga, s/n, 08907 L'Hospitalet del Llobregat, Barcelona, Spain; Tel: +34 (93) 402 4280/ +34 (93) 403 5820; Fax: +34 (93) 402 9082; E-mail: fciruela@ub.edu


Abstract

The existence of a supramolecular organization of the G protein-coupled receptor (GPCR) is now being widely accepted by the scientific community. Indeed, GPCR oligomers may enhance the diversity and performance by which extracellular signals are transferred to the G proteins in the process of receptor transduction, although the mechanism that underlies this phenomenon still remains unsolved. Recently, it has been proposed that a trans-conformational switching model could be the mechanism allowing direct inhibition/activation of receptor activation/inhibition, respectively. Thus, heterotropic receptor-receptor allosteric regulations are behind the GPCR oligomeric function. In this paper we want to revise how GPCR oligomerization impinges on several important receptor functions like biosynthesis, plasma membrane diffusion or velocity, pharmacology and signaling. In particular, the rationale of receptor oligomerization might lie in the need of sensing complex whole cell extracellular signals and translating them into a simple computational model.

Keywords: G protein-coupled receptor, protein-protein interaction, GPCR oligomerization.