Method for Determining the Activity of a Protease in a Sample
    5.
    发明申请
    Method for Determining the Activity of a Protease in a Sample 审中-公开
    测定样品中蛋白酶活性的方法

    公开(公告)号:US20100021940A1

    公开(公告)日:2010-01-28

    申请号:US12296568

    申请日:2007-04-11

    CPC classification number: C12Q1/37 G01N2333/96486 G01N2500/00 G01N2800/122

    Abstract: There is provided a method for determining the activity of a protease in a sample. The method comprises (i) admixing said sample with a substrate, wherein the substrate has the formula (1a) wherein: R1 is a hydrocarbyl group; R2 is a first peptide moiety; R3 is a second peptide moiety and X is selected from the group consisting of O, S and NH; Y1 is a suitable substituent; Y2 is a suitable substituent; and (ii) determining the activity of said protease by detecting the presence of a reporter having the formula H—X—R1, wherein: X is selected from the group consisting of O, S and NH; R1 is a hydrocarbyl group. The substrate and reporter are useful for determining the efficacy of protease-modulators and candidate protease-modulators and in the diagnosis of a disease or disorder in a subject.

    Abstract translation: 提供了测定样品中蛋白酶活性的方法。 该方法包括(i)将所述样品与基底混合,其中基底具有式(1a),其中:R1是烃基; R2是第一个肽部分; R3是第二肽部分,X选自O,S和NH; Y1是合适的取代基; Y2是合适的取代基; 和(ii)通过检测存在具有式H-X-R1的报告基来确定所述蛋白酶的活性,其中:X选自O,S和NH; R1是烃基。 底物和报告物可用于确定蛋白酶调节剂和候选蛋白酶调节剂的功效以及受试者中疾病或病症的诊断。

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