Application of BRET to monitor ligand binding to GPCRs.

Stoddart, Leigh A; Johnstone, Elizabeth K M; Wheal, Amanda J; Goulding, Joëlle; Robers, Matthew B; Machleidt, Thomas; Wood, Keith V; Hill, Stephen J et al. · Nat Methods · 2015

basic_science · Level V

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Abstract

Bioluminescence resonance energy transfer (BRET) is a well-established method for investigating protein-protein interactions. Here we present a BRET approach to monitor ligand binding to G protein-coupled receptors (GPCRs) on the surface of living cells made possible by the use of fluorescent ligands in combination with a bioluminescent protein (NanoLuc) that can be readily expressed on the N terminus of GPCRs.

Medical subject headings