Journal
CURRENT OPINION IN CHEMICAL BIOLOGY
Volume 9, Issue 5, Pages 517-525Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.cbpa.2005.08.016
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- Wellcome Trust Funding Source: Medline
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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 readouts 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.
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