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Megan Hogan, Medhanit Bahta, Scott Cherry, George T. Lountos, Joseph E. Tropea, Bryan M. Zhao, Terrence R. Burke Jr, David S. Waugh and Robert G. Ulrich Biomolecular Interactions of Small-molecule Inhibitors Affecting the YopH Protein Tyrosine Phosphatase Chemical Biology & Drug Design 81

Article first published online: 13 FEB 2013 | DOI: 10.1111/cbdd.12097

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We have developed competitive and direct binding methods to examine small-molecule inhibitors of protein tyrosine phosphatase (PTPase) activity. Focusing on the Yersinia outer protein H (YopH), a potent bacterial PTPase, we describe how an understanding of the kinetic interactions involving YopH, peptide substrates, and small-molecule inhibitors of PTPase activity can be beneficial for inhibitor screening and we further translate these results into a microarray assay for high-throughput screening.

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