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) (PMID:19309353) (PMCID:PMC2795239)

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 > School of Psychology & Neuroscience
• 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 Code	Award No	Project Name	Principal Investigator	Funder's Name	Funder Ref	Lead Dept
43705	1	Exploring the selectivity and consequences of GPCR homo and hetero dimerisation/oligomerisation using receptors activated solely by ......	Graeme Milligan	Biotechnology and Biological Sciences Research Council (BBSRC)	BB/E006302/1	Institute of Neuroscience and Psychology
40463	1	The molecular basis of cannabinoid CB1 receptor regulation of the sensitivity of orexin-1 receptor signalling	Graeme Milligan	Biotechnology and Biological Sciences Research Council (BBSRC)	BB/D001951/1	Institute of Neuroscience and Psychology
38978	1	The quaternary structure of G-protein coupled receptors - implications for function drug design. Programme grant support renewal	Graeme Milligan	Medical Research Council (MRC)	G9811527	Institute of Neuroscience and Psychology
40094	1	The existence and functional importance of interactions between opiod receptors and the CXCR1/2 chemokine receptors	Graeme Milligan	Wellcome Trust (WELLCOME)	076774/Z/05/Z	Institute of Neuroscience and Psychology