L. Kallal et Jl. Benovic, Using green fluorescent proteins to stud G-protein-coupled receptor localization and trafficking, TRENDS PHAR, 21(5), 2000, pp. 175-180
G-protein-coupled receptors (GPCRs) mediate a diverse array of biological f
unctions as a result of their ability to respond selectively to extra cellu
lar stimuli, which ultimately results in cell-specific activation of signal
ing cascades. Generally, GPCR activation is followed rapidly by a loss of r
esponsiveness, termed desensitization, which is then followed by a period o
f recovery or resensitization, These changes in signaling potential are tig
htly regulated, primarily via mechanisms that involve GPCR phosphorylation
and trafficking to distinct locations within the cell. Tagging of GPCRs wit
h the green fluorescent protein (GFP) has enabled the direct visualization
of real-time trafficking of GPCRs in living cells. Such analyses have provi
ded crucial insight into the mechanisms involved in controlling GPCR functi
on.