Artigo Acesso aberto Revisado por pares

Application of BRET to monitor ligand binding to GPCRs

2015; Nature Portfolio; Volume: 12; Issue: 7 Linguagem: Inglês

10.1038/nmeth.3398

ISSN

1548-7105

Autores

Leigh A. Stoddart, Elizabeth K. M. Johnstone, Amanda J. Wheal, Joëlle Goulding, Matthew B. Robers, Thomas Machleidt, Keith V. Wood, Stephen J. Hill, Kevin D. G. Pfleger,

Tópico(s)

Photoreceptor and optogenetics research

Resumo

Bioluminescence resonance energy transfer, from the substrate of a luciferase fused with a G protein–coupled receptor to a fluorescent dye covalently linked to a receptor ligand, allows the profiling of ligand affinity and binding kinetics. 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.

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