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2015PNAS文章online(五年影响因子 10.563)

文章来源:  |  发布时间:2015-04-20  |  作者:  |  浏览次数:  |  【打印】 【关闭

 

Discovery of an intrinsic tenase complex inhibitor: Pure nonasaccharide from fucosylated glycosaminoglycan

  与赵金华,刘吉开课题组合作,世界上首次发表内源性凝血因子X酶(FXase)的选择性抑制寡糖-nonasaccharides!

  其优势非常明显,能显著降低出血倾向,而抑制血栓形成的作用与低分子肝素相当,是一个非常有前景的先导化合物;后续工作正在进行,欢迎加入this project!

  英文摘要如下:全文链接 click 

Significance

      Selective inhibition of the intrinsic coagulation pathway is a promising strategy for developing safer anticoagulants without serious bleeding consequences. We prepared and identified a series of oligosaccharides as inhibitors of the intrinsic tenase, which is the final and rate-limiting enzyme complex in the intrinsic coagulation pathway and is an attractive but less explored target for anticoagulants due to the lack of a pure selective inhibitor. Analysis of these purified oligosaccharides reveals the precise structure of fucosylated glycosaminoglycan. Among these oligosaccharides, nonasaccharide is the minimum fragment that retains potent anticoagulant activity by selective inhibition of the intrinsic tenase while avoiding adverse effects and, thus, it may pave the way for the development of better treatments for thromboembolic diseases.


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