The BRET technology and its application to screening assays

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Biological Assay / trends*
  • Drug Design*
  • Fluorescence Resonance Energy Transfer / trends*
  • Luminescent Measurements / trends*
  • Luminescent Proteins*
  • Protein Interaction Mapping / methods*


  • Luminescent Proteins