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

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

Author information

1
Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK G12 8QQ. g.milligan@bio.gla.ac.uk

Abstract

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.

PMID:
10637652
DOI:
10.1016/s0165-6147(99)01404-2
[Indexed for MEDLINE]

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