Overview

Recent advancements in site-directed labeling of G protein-coupled receptors (GPCRs) and interacting proteins with fluorescent probes such as variants of the green fluorescent proteins (GFP) and small fluorescent molecules enabled detailed studies of receptor function. In the context of developments in fluorescence spectroscopy and life cell imaging, a considerable amount of new insights into the dynamics and extent of ligand-induced conformational changes of receptors have been achieved. This chapter discusses details of how to label a GPCR with different fluorescent dyes, it highlights advantages and disadvantages of fluorescence resonance energy transfer (FRET) and bioluminescence resonance energy transfer (BRET) in order to study protein conformations as well as protein-protein interactions, and also contains some advice of when and how to use these techniques in order to study receptor function.

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