Bioluminescence Resonance Energy Transfer ( BRET ) Technologies to Study GPCRs

G protein-coupled receptors (GPCRs) represent a major target for the development of pharmaceuticals. As such, they are subject to extensive research to understand their function, as well as how their signaling is influenced by therapeutics. Bioluminescence Resonance Energy Transfer (BRET) is a biophysical technique that enables real-time monitoring of protein and small molecule proximity in live cells. BRET has seen widespread use as an important research tool to elucidate many aspects of GPCR pharmacology. Recently, multiple technological advances have furthered the scope and power of BRET techniques. New assay platforms such as NanoBRET have enabled the development of novel applications of the BRET technique, while the combination of BRET with newly developed biosensors has been shown to be a powerful research strategy. Here, we review recent BRET assay developments and their uses, demonstrating the rapidly expanding facets of GPCR pharmacology that can be studied utilizing BRET technologies. These tools will likely prove to be fundamental in furthering our understanding of GPCR function and pharmaceutical development.