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Updated: May 23, 2026

A Rapid and Quantitative Fluorimetric Method for Protein-Targeting Small Molecule Drug Screening
Published on: October 16, 2015
Supramolecular displacement-mediated activation of a silent fluorescence probe for label-free ligand screening
Diego Amado Torres1, Malar A Azagarsamy, S Thayumanavan
1Department of Chemistry, University of Massachusetts at Amherst, Amherst, Massachusetts 01003, USA.
Abstract:
We report a new approach for the rapid screening of analyte binding affinities for a target protein. We demonstrate that a molecular probe, with a pro-fluorophore substrate and ligand moieties, can be hindered from enzymatic access when bound to the target protein. When analytes displace the probe from the protein's binding pocket, a fluorescence profile is generated. This profile is used to discriminate analytes based on their relative binding affinities.
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