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Br J Pharmacol. 2019 Dec 26. doi: 10.1111/bph.14953. [Epub ahead of print]

Fluorescent ligands: Bringing light to emerging G protein-coupled receptor paradigms.

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Cell Signalling and Pharmacology Research Group, Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.


In recent years several novel aspects of G protein-coupled receptor (GPCR) pharmacology have been described, which are thought to play a role in determining the in vivo efficacy of a compound. Fluorescent ligands have been used to study many of these, which have also required the development of new experimental approaches. Fluorescent ligands offer the potential to use the same fluorescent probe to perform a broad range of experiments, from single molecule microscopy to in vivo bioluminescence resonance energy transfer. This review provides an overview of the in vitro use of fluorescent ligands in further understanding emerging pharmacological paradigms within the GPCR field, including ligand binding kinetics, allosterism and intracellular signalling, along with the use of fluorescent ligands to study physiologically relevant therapeutics.


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