Alternative technique for assessing binding kinetics in live cells

Researchers have recently demonstrated, 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).

Published in the journal Nature Methods, 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 combines the knowledge and expertise of the laboratories of Associate Professor Kevin Pfleger of The University of Western Australia/Harry Perkins Institute of Medical Research and Professor Stephen Hill of The University of Nottingham (UK), who are leaders in BRET and fluorescence technology development respectively; the latest reagents and developmental know-how from Promega (USA); and the high-throughput microplate reader instrumentation and associated expertise from BMG LABTECH (Australia).

The paper is a major outcome of an Australian Research Council Linkage Grant that is targeted towards developing new technological approaches enabling academics and biotech and pharmaceutical companies to discover novel treatments for a range of disorders.