Stoddart et al. propose rational design of a covalent and selective ligand probe to fluorescently label GPCR in transiently transfected and endogenous systems. Using the adenosine A2A receptor as a model system, they show fluorescent labelling in an endogenous system, without impeding access to the orthosteric binding site. This study is useful to selectively and non-invasively study localisation and functions of GPCRs.
- Leigh A. Stoddart
- Nicholas D. Kindon
- Barrie Kellam