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    Assays for protease enzyme activity
    3.
    发明申请
    Assays for protease enzyme activity 审中-公开
    蛋白酶活性测定

    公开(公告)号：US20050014160A1

    公开(公告)日：2005-01-20

    申请号：US10621311

    申请日：2003-07-18

    申请人： Sriram Kumaraswamy ,  Komandoor Achyuthan ,  Xiaobo Shi ,  Troy Bergstedt ,  Frauke Rininsland ,  Duncan McBranch ,  David Whitten

    发明人： Sriram Kumaraswamy ,  Komandoor Achyuthan ,  Xiaobo Shi ,  Troy Bergstedt ,  Frauke Rininsland ,  Duncan McBranch ,  David Whitten

    IPC分类号： C07H21/04 ,  C12Q1/37 ,  C12Q1/68 ,  G01N33/53

    CPC分类号： B82Y20/00 ,  B82Y5/00 ,  B82Y10/00 ,  C07H21/04 ,  C09B11/24 ,  C09B69/105 ,  C12Q1/37 ,  C12Q2337/00

    摘要： Bioconjugates, kits and assays for detecting the activity of protease enzymes such as β-secretase and caspase enzymes are described. The bioconjugates include a tether having a segment capable of recognizing and interacting with (e.g., being cleaved by) the enzyme, a fluorescer including a plurality of fluorescent species conjugated to a first location on the tether, and a quencher conjugated to a second location on the tether. The segment capable of recognizing and interacting with the protease enzyme (e.g., β-secretase or caspase) is located between the first and second locations on the tether. The plurality of fluorescent species are associated with one another such that the quencher is capable of amplified super-quenching of the fluorescer. The assay is suitable for screening potential drugs for their efficiency in inhibiting the activity of protease enzymes such as β-secretase in a high throughput format where the potential drugs are evaluated.

    摘要翻译： 描述了用于检测蛋白酶如β-分泌酶和半胱天冬酶的活性的生物缀合物，试剂盒和测定法。 生物缀合物包括具有能够识别并与酶相互作用（例如被切割）的区段的系链，包含与系链上的第一位置缀合的多个荧光物质的荧光剂，以及与第二位置缀合的猝灭剂 系绳 能够识别和与蛋白酶（例如，β-分泌酶或胱天蛋白酶）相互作用的区段位于系链上的第一和第二位置之间。 多个荧光物质彼此相关联，使得猝灭剂能够扩增荧光剂的超猝灭。 该测定法适用于筛选潜在药物在抑制潜在药物评估的高通量形式中蛋白酶如β-分泌酶的活性的效率。