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Chinese Journal of Antibiotics. 2018, (06)

Discovery of flavoglaucin as an inhibitor of PTP-Shp2Chinese Full Text

Zhang Xue-lian;Zheng Hai-zhou;Xu Yan;Lu Xin-hua;Zhu Jing-tong;Zheng Zhi-hui;New Drug Research ＆ Development Limited Company of North China Pharmaceutical Group Corporation,National Microbial Medicine Engineering ＆ Research Center,Industry Microorganism Metabolites Engineering Technology of Hebei ＆ Research Center,Shijiazhuang Engineering Laboratory for New Drugs Screening;

Abstract: Objective To discover small molecule inhibitors of protein tyrosine phosphatase Shp2（PTP-Shp2）. Methods We used a high-throughput screening method to find small molecular inhibitors of PTP-Shp2 and kinetic analysis of Shp2 inhibition was implemented. We assessed the inhibitor binding sites in Shp2 using molecular docking. Results In this study, flavoglaucin was identified as a Shp2 inhibitor from products of microbial metabolism in our lab by a high-throughput screening method with an IC50<... More
Keywords：

PTP-Shp2; Inhibitor; Flavoglaucin;

  • DOI：

    10.13461/j.cnki.cja.006276

  • Series：

    (E) Medicine ＆ Public Health

  • Subject：

    Pharmaceutics

  • Classification Code：

    R915

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