Fluorophore-tagged GPCR ligands.
Fluorescently tagged drug molecules can be successfully employed to visualize the location of their receptor target at the single-cell level. Furthermore, if their binding to the receptor is reversible, one can now obtain detailed pharmacological information such as affinity using single-molecule detection techniques. When coupled to the growing exploitation of fluorescence-based read-outs in high throughput and high content screening, it is clear that fluorescent molecules offer a safer, more powerful and more versatile alternative to radioligands in molecular pharmacology and drug discovery. GPCR pharmacology has benefited enormously from the application of fluorescence-based technologies and we now possess a much greater understanding of this receptor family's basic molecular mechanisms of action through the careful design and judicious use of fluorescent peptide and small-molecule-based ligands.
Middleton
Richard J
RJ
School of Pharmacy, Centre for Biomolecular Sciences, University of Nottingham, Nottingham NG7 2RD, UK.
Kellam
Barrie
B
D005456:Fluorescent Dyes / Q000737:chemistry*; D008024:Ligands; D018102:Receptors, Leukotriene B4 / Q000737:chemistry*; D018048:Receptors, Purinergic P2 / Q000737:chemistry*
D005456:Fluorescent Dyes; D008024:Ligands; D018102:Receptors, Leukotriene B4; D018048:Receptors, Purinergic P2