The efficiency of interactions between G-pratein-coupled receptors (GPCRs)
and heterotrimeric guanine nucleotide-binding proteins (G proteins) is grea
tly influenced by the absolute and relative densities of these proteins in
the plasma membrane. The study of these interactions has been facilitated b
y the use of GPCR-G alpha fusion proteins, which are formed by the fusion o
f GPCR to Ga. These fusion proteins ensure a defined 1:1 stoichiometry of G
PCR to GOL and force the physical proximity of the signalling partners. Thu
s, fusion of GPCR to G alpha enhances coupling efficiency can be used to st
udy aspects of receptor-G-protein coupling that could not otherwise be exam
ined by co-expressing GPCRs and G proteins as separate proteins. The result
s of studies that have made use of GPCR-G alpha fusion proteins will be dis
cussed in this article, along with the strengths and limitations of this ap
proach.