The BRET technology and its application to screening assays

The bioluminescence resonance energy transfer (BRET) method is based on resonance energy transfer between a light‐emitting enzyme and a fluorescent acceptor. Since its first description in 1999, several versions of BRET have been described using different substrates and energy donor/acceptor couples. Today, BRET is considered as one of the most versatile techniques for studying the dynamics of protein‐protein interactions in living cells. Various studies have applied BRET‐based assays to screen new receptor ligands and inhibitors of disease‐related‐proteases. Inhibitors of protein‐protein interactions are likely to become a new major class of therapeutic drugs, and BRET technology is expected to play an important role in the identification of such compounds. This review describes the original BRET‐based methodology, more recent variants, and potential applications to drug screening.

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