title: The BRET technology and its application to screening assays.
abstract: 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.
authors.affiliation: UMR 8090, CNRS, Université Lille 2, Lille, France.
authors.forename: Johan
authors.initials: J
authors.lastname: Bacart
authors.forename: Caroline
authors.initials: C
authors.lastname: Corbel
authors.forename: Ralf
authors.initials: R
authors.lastname: Jockers
authors.forename: Stéphane
authors.initials: S
authors.lastname: Bach
authors.forename: Cyril
authors.initials: C
authors.lastname: Couturier
mesh_terms: D001681:Biological Assay / Q000639:trends*; D015195:Drug Design; D031541:Fluorescence Resonance Energy Transfer / Q000639:trends*; D008163:Luminescent Measurements / Q000639:trends*; D008164:Luminescent Proteins; D025941:Protein Interaction Mapping / Q000379:methods*
chemical_list: D008164:Luminescent Proteins