Bacart Johan, Corbel Caroline, Jockers Ralf, Bach Stéphane, Couturier Cyril
UMR 8090, CNRS, Université Lille 2, Lille, France.
Biotechnol J. 2008 Mar;3(3):311-24. doi: 10.1002/biot.200700222.
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.
生物发光共振能量转移（BRET）方法基于发光酶与荧光受体之间的共振能量转移。自1999年首次被描述以来，已经出现了几个使用不同底物以及能量供体/受体对的BRET版本。如今，BRET被认为是研究活细胞中蛋白质-蛋白质相互作用动态的最通用技术之一。各种研究已应用基于BRET的检测方法来筛选新的受体配体和疾病相关蛋白酶的抑制剂。蛋白质-蛋白质相互作用的抑制剂很可能成为一类新的主要治疗药物，并且预计BRET技术将在这类化合物的鉴定中发挥重要作用。这篇综述描述了基于BRET的原始方法、最新变体以及在药物筛选中的潜在应用。
