The field of G protein-coupled receptor (GPCR) research has undergone a transformation in recent years due to the notion of heteromerization. In order to progress our understanding of the functional implications of this phenomenon, as well as its applicability across the diversity of GPCR subtypes, we need to continually look to improve the technologies we use to evaluate protein-protein interactions in as near a physiological setting as possible. The bioluminescence resonance energy transfer (BRET) technology has been intimately associated with the study of GPCR-GPCR interactions for the past ten years, and over this period, both the tools and the methods of analysis have continually evolved. In this review, we highlight recent advances in the BRET technology and focus particularly on the drive to establish the specificity of GPCR heteromers.
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