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Application of BRET to monitor ligand binding to GPCRs

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

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Leigh A. Stoddart

Elizabeth K.M. Johnstone

Amanda J. Wheal

Matthew B. Robers

Thomas Machleidt

Keith V. Wood

Professor of Molecular Pharmacology

Kevin D.G. Pfleger


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.


Stoddart, L. A., Johnstone, E. K., Wheal, A. J., Goulding, J., Robers, M. B., Machleidt, T., …Pfleger, K. D. (in press). Application of BRET to monitor ligand binding to GPCRs. Nature Methods, 12,

Journal Article Type Article
Acceptance Date Apr 4, 2015
Online Publication Date Jun 1, 2015
Deposit Date Jul 19, 2016
Publicly Available Date Jul 19, 2016
Journal Nature Methods
Print ISSN 1548-7091
Electronic ISSN 1548-7105
Publisher Nature Publishing Group
Peer Reviewed Peer Reviewed
Volume 12
Keywords cell signalling, drug development, optical spectroscopy
Public URL
Publisher URL
Contract Date Jul 19, 2016


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