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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; PTPN1) 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

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Schneider, R. et al. J. Am. Chem. Soc.; published online April 23, 2013;
doi:10.1021/ja4030484
Contact: Daniel Rauh, Technical University of Dortmund, Dortmund, Germany
e-mail:
daniel.rauh@tu-dortmund.de