G protein-coupled receptor dimerization: function and ligand pharmacology.
It is now generally accepted that G protein-coupled receptors (GPCRs) can exist as dimers or as part of larger oligomeric complexes. Increasing evidence suggests that a dimer is the minimal functional structure, but considerable variation exists between reports of the effects of agonist ligands on quaternary structure. Many studies have intimated the existence of heterodimeric GPCR pairings. Key questions that remain to be addressed effectively include the prevalence and relevance of these in native tissues and the implications of heterodimerization for pharmacology and, potentially, for drug design.
Milligan
Graeme
G
Molecular Pharmacology Group, Davidson Building, University of Glasgow, Glasgow G12 8QQ Scotland, UK. g.milligan@bio.gla.ac.uk
D000818:Animals; D019281:Dimerization; D006801:Humans; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects / Q000378:metabolism*
D008024:Ligands; D043562:Receptors, G-Protein-Coupled