Thursday, May 23, 2013
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Assays & screens
Fluorescence labels in
phosphatase (FLiP) assay to detect allosteric inhibitors of phosphatases
A FLiP assay could help
identify allosteric inhibitors of phosphatases. An allosteric inhibitor of protein
tyrosine phosphatase 1B (PTP-1B;
bound a pocket about 20 Å from the enzyme's active site and blocked
phosphatase activity by displacing the a7 helix from the
phosphatase core. A high throughput FLiP assay was created by labeling the
PTP-1B a7 helix with a red fluorophore, which produced
altered emission spectra when displaced. In this assay, the allosteric
inhibitor shifted the emission spectra readout, whereas an active site-targeting
inhibitor or nonbinding control molecule did not. Next steps could include
using the screen to identify additional phosphatase inhibitors.
SciBX 6(20); doi:10.1038/scibx.2013.498
Published online May 23, 2013
Patent and licensing status
Schneider, R. et al. J.
Am. Chem. Soc.; published online April 23, 2013;
Contact: Daniel Rauh, Technical University of Dortmund, Dortmund,
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