A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase, YopH
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- 作者：Fa Liu ; Ramin Mollaaghababa Hakami ; Beverly Dyas ; Medhanit Bahta ; George T. Lountos ; David S. Waugh ; Robert G. Ulrich ; Terrence R. Burke Jr.
- 关键词：Protein-tyrosine phosphatase ; Yersinia pestis ; YopH ; Inhibitor
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：1 May 2010
- 年：2010
- 卷：20
- 期：9
- 页码：2813-2816
- 全文大小：436 K
文摘
A bivalent tethered approach toward YopH inhibitor development is presented that joins aldehydes with mixtures of bis-aminooxy-containing linkers using oxime coupling. The methodology is characterized by its facility and ease of use and its ability to rapidly identify low micromolar affinity inhibitors. The generality of the approach may potentially make it amenable to the development of bivalent inhibitors directed against other phosphatases.