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Trends Pharmacol Sci. 2000 Jan;21(1):24-8.

Insights into ligand pharmacology using receptor-G-protein fusion proteins.

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Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK G12 8QQ.


Production of chimeric DNAs in which the 5' end of G-protein alpha-subunits are linked directly to the 3' tail of a G-protein-coupled receptor has recently offered an unusual strategy to explore the detailed pharmacology of receptor-G-protein interactions. Expression of such fusion proteins ensures a 1:1 stoichiometry of receptor and G-protein expression and their proximity to each other. The capacity of such fusion proteins to be regarded as agonist-activated GTPases that allow simple enzyme kinetics to be applied to issues of ligand efficacy will be considered. In addition, the effects of point mutations, in both receptors and G proteins, on ligand function are particularly amenable to the types of robust quantitative analyses that can be produced using such fusion proteins.

[Indexed for MEDLINE]

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