The use of receptor G-protein fusion proteins for the study of ligand activity.
Fusion proteins in which the N-terminus of a G protein alpha subunit is attached in frame to the C-terminal tail of a G-protein-coupled receptor have become widely used as experimental systems to explore the quantitative details of ligand stimulation of specific receptor G-protein combinations. In part, this reflects that they function as agonist-activated GTPases that behave with simple Michaelan kinetics. They have also been used to explore the effects of mutation in both receptor and G protein on information transfer, ligand regulation of posttranslational acylation, and the mechanism and potential selectivity of regulators of G-protein signaling.
Milligan
Graeme
G
Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK. g.milligan@bio.gla.ac.uk
D000818:Animals; D019556:COS Cells; D004305:Dose-Response Relationship, Drug; D019204:GTP-Binding Proteins / Q000737:chemistry* / Q000378:metabolism; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008024:Ligands; D009154:Mutation; D010169:Palmitic Acids / Q000378:metabolism; D011110:Polymorphism, Genetic; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D011993:Recombinant Fusion Proteins / Q000378:metabolism; D015398:Signal Transduction
D008024:Ligands; D010169:Palmitic Acids; D011993:Recombinant Fusion Proteins; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D019204:GTP-Binding Proteins