Biomolecular Interactions of Small-molecule Inhibitors Affecting the YopH Protein Tyrosine Phosphatase (pages 323–333)
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
Article first published online: 13 FEB 2013 | DOI: 10.1111/cbdd.12097
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.