According to BMG LABTECH, the paper, entitled “Application of BRET to monitor ligand binding to GPCRs,” demonstrates for the first time the principle of real-time ligand binding to G-protein-coupled receptors (GPCRs), the single most important family of drug targets, using bioluminescence resonance energy transfer (BRET). In effect, the company says, the BRET technique has been shown to be an alternative to radio ligand binding experiments and extends researchers’ capability to allow assessment of real-time binding kinetics in live cells. This adds to the established capability of BRET to monitor protein-protein interactions in real time in live cells, further enhancing biologists’ and pharmacologists’ insights into real-time cellular processes.

 

The project combined the knowledge and expertise of the laboratories of Kevin Pfleger of The University of Western Australia/Harry Perkins Institute of Medical Research and Stephen Hill of The University of Nottingham, who are leaders in BRET and fluorescence technology development respectively. All BRET measurements shown in the paper were performed on BMG LABTECH’s multimode microplate readers CLARIOstar and PHERAstar FS.