小分子抑制剂对 YopH 蛋白酪氨酸磷酸酶的生物分子相互作用。
Biomolecular Interactions of small-molecule inhibitors affecting the YopH protein tyrosine phosphatase.
机构信息
United States Army Medical Research Institute of Infectious Diseases, Frederick, MD 21702, USA.
出版信息
Chem Biol Drug Des. 2013 Mar;81(3):323-33. doi: 10.1111/cbdd.12097.
Abstract
We have developed competitive and direct binding methods to examine small-molecule inhibitors of protein tyrosine phosphatase activity. Focusing on the Yersinia pestis outer protein H, a potent bacterial protein tyrosine phosphatase, we describe how an understanding of the kinetic interactions involving Yersinia pestis outer protein H, peptide substrates, and small-molecule inhibitors of protein tyrosine phosphatase activity can be beneficial for inhibitor screening, and we further translate these results into a microarray assay for high-throughput screening.
摘要
我们已经开发出竞争性和直接结合方法来检测蛋白酪氨酸磷酸酶活性的小分子抑制剂。本文以鼠疫耶尔森氏菌外蛋白 H 为研究对象，该蛋白是一种有效的细菌蛋白酪氨酸磷酸酶，我们描述了如何理解涉及鼠疫耶尔森氏菌外蛋白 H、肽底物和蛋白酪氨酸磷酸酶活性小分子抑制剂的动力学相互作用，这将有利于抑制剂筛选，并且我们进一步将这些结果转化为高通量筛选的微阵列测定法。
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