Apr 23, 2020

Ligand-directed covalent labelling of a GPCR with a fluorescent tag

BioRxiv : the Preprint Server for Biology
L. A. StoddartB. Kellam


Here, we describe rational design of a compound that covalently and selectively labels a G protein-coupled receptor (GPCR) in living cells with a fluorescent moiety. Using wild-type adenosine A2A receptor as a model system, we show fluorescent labelling without impeding access to the orthosteric binding site and demonstrate its use in endogenously expressing systems. This offers a non-invasive and selective approach to study function and localisation of native GPCRs.

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Mentioned in this Paper

Genetic Disorders Screening
Cell Growth
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