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Int. J. Mol. Sci. 2014, 15(3), 4856-4877; doi:10.3390/ijms15034856

Dimers of G-Protein Coupled Receptors as Versatile Storage and Response Units

Department of Microbiology and Molecular Cell Sciences, University of Memphis, Memphis, TN 38152, USA
Department of Psychiatry, University of Cincinnati School of Medicine, Cincinnati, OH 45267, USA
Department of Surgery, University of Cincinnati School of Medicine, Cincinnati, OH 45267, USA
Department of Pharmacology, University of Tennessee Health Science Center, Memphis, TN 38163, USA
Author to whom correspondence should be addressed.
Received: 7 January 2014 / Revised: 28 February 2014 / Accepted: 4 March 2014 / Published: 19 March 2014
(This article belongs to the Collection G Protein-Coupled Receptor Signaling and Regulation)
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The status and use of transmembrane, extracellular and intracellular domains in oligomerization of heptahelical G-protein coupled receptors (GPCRs) are reviewed and for transmembrane assemblies also supplemented by new experimental evidence. The transmembrane-linked GPCR oligomers typically have as the minimal unit an asymmetric ~180 kDa pentamer consisting of receptor homodimer or heterodimer and a G-protein αβγ subunit heterotrimer. With neuropeptide Y (NPY) receptors, this assembly is converted to ~90 kDa receptor monomer-Gα complex by receptor and Gα agonists, and dimers/heteropentamers are depleted by neutralization of Gαi subunits by pertussis toxin. Employing gradient centrifugation, quantification and other characterization of GPCR dimers at the level of physically isolated and identified heteropentamers is feasible with labeled agonists that do not dissociate upon solubilization. This is demonstrated with three neuropeptide Y (NPY) receptors and could apply to many receptors that use large peptidic agonists. View Full-Text
Keywords: heteropentamer; G-protein heterotrimer; heterodimer; homodimer heteropentamer; G-protein heterotrimer; heterodimer; homodimer

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Parker, M.S.; Sah, R.; Balasubramaniam, A.; Park, E.A.; Sallee, F.R.; Parker, S.L. Dimers of G-Protein Coupled Receptors as Versatile Storage and Response Units. Int. J. Mol. Sci. 2014, 15, 4856-4877.

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