Journal
ANALYTICAL CHEMISTRY
Volume 95, Issue 5, Pages 2848-2856Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.analchem.2c04269
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By conjugating the Py-5 fluorophore with mirabegron using a polyethylene glycol (PEG) chain, we have developed a highly selective fluorescent ligand, H2, for fl3-AR. H2 rapidly releases turn-on fluorescent signals when incubated with fl3-AR, enabling quick and accurate identification at different levels.
For the precise visualization of GPCR, subtype selectivity of turn-on fluorescent ligands is of major relevance. Although there are many thriving fl-adrenergic receptors (fl-ARs) probes, none of them are selective to the fl3-subtype, which severely limits the development of fl3-AR investigations. Using a polyethylene glycol (PEG) chain to conjugate the Py-5 fluorophore with mirabegron, we present here a highly selective fluorescent ligand, H2, for fl3-AR. It was established by the radioligand and NanoLuc-based bioluminescence resonance energy transfer (NanoBRET) binding experiments that molecule H2 has a substantially higher affinity for fl3-AR than the other two subtypes (1/3, 45-fold; 2/3, 16-fold). More crucially, when molecule H2 was incubated with fl3-AR, the turn-on fluorescent signals could be quickly released. The subsequent investigations, which included cell imaging, tissue imaging, and flow-cytometry analysis, proved that molecule H2 may make it possible to quickly and accurately fluorescently identify fl3-AR at different levels. We offer a prospective fluorescent turn-on ligand with exceptional selectivity for fl3-AR as a result of our combined efforts.
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