G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function

Milligan, G. (2009) G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function. British Journal of Pharmacology, 158(1), pp. 5-14. (doi:10.1111/j.1476-5381.2009.00169.x)

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Publisher's URL: http://dx.doi.org/10.1111/j.1476-5381.2009.00169.x

Abstract

The concept that G protein-coupled receptors (GPCRs) can form hetero-dimers or hetero-oligomers continues to gain experimental support. However, with the exception of the GABAB receptor and the sweet and umami taste receptors few reported examples meet all of the criteria suggested in a recent International Union of Basic and Clinical Pharmacology sponsored review (Pin et al., 2007) that should be required to define distinct and physiologically relevant receptor species. Despite this, there are many examples in which pairs of co-expressed GPCRs reciprocally modulate their function, trafficking and/or ligand pharmacology. Such data are at least consistent with physical interactions between the receptor pairs. In recent times, it has been suggested that specific GPCR hetero-dimer or hetero-oligomer pairs may represent key molecular targets of certain clinically effective, small molecule drugs and there is growing interest in efforts to identify ligands that may modulate hetero-dimer function selectively. The current review summarizes key recent developments in these topics.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Milligan, Professor Graeme
Authors: Milligan, G.
College/School:College of Medical Veterinary and Life Sciences > Institute of Neuroscience and Psychology
Journal Name:British Journal of Pharmacology
Journal Abbr.:BJP
Publisher:John Wiley & Sons Ltd.
ISSN:0007-1188
ISSN (Online):1476-5381
Published Online:20 March 2009
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Project CodeAward NoProject NamePrincipal InvestigatorFunder's NameFunder RefLead Dept
437051Exploring the selectivity and consequences of GPCR homo and hetero dimerisation/oligomerisation using receptors activated solely by ......Graeme MilliganBiotechnology and Biological Sciences Research Council (BBSRC)BB/E006302/1Institute of Neuroscience and Psychology
404631The molecular basis of cannabinoid CB1 receptor regulation of the sensitivity of orexin-1 receptor signallingGraeme MilliganBiotechnology and Biological Sciences Research Council (BBSRC)BB/D001951/1Institute of Neuroscience and Psychology
389781The quaternary structure of G-protein coupled receptors - implications for function drug design. Programme grant support renewalGraeme MilliganMedical Research Council (MRC)G9811527Institute of Neuroscience and Psychology
400941The existence and functional importance of interactions between opiod receptors and the CXCR1/2 chemokine receptorsGraeme MilliganWellcome Trust (WELLCOME)076774/Z/05/ZInstitute of Neuroscience and Psychology