Journal
JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION
Volume 29, Issue 3-4, Pages 163-172Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/10799890903079844
Keywords
Label-free; signaling; seven-transmembrane receptor; high throughput screening
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Seven-transmembrane receptors (7TMRs) are a family of proteins of great interest as therapeutic targets because of their abundance on the cell surface, diverse effects in modulating cell behavior and success as a key class of drugs. We have evaluated the Epic (R) label-free system for the purpose of identifying antagonists of the muscarinic M3 receptor. We compared the data generated from the label-free technology with data for the same compounds in a calcium flux assay. We have shown that this technology can be used for high throughput screening (HTS) of 7TMRs and as an orthogonal approach to enable rapid evaluation of HTS outputs. A number of compounds have been identified which were not found in a functional HTS measuring the output from a single pathway, which may offer new approaches to inhibiting responses through this receptor.
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