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    • 6. 发明授权
    • Method for assaying histone methylation enzyme activity
    • 测定组蛋白甲基化酶活性的方法
    • US09012166B2
    • 2015-04-21
    • US13639334
    • 2011-04-15
    • Norikazu NishinoYasushi TakemotoAkihiro ItoMinoru Yoshida
    • Norikazu NishinoYasushi TakemotoAkihiro ItoMinoru Yoshida
    • G01N21/78C12Q1/37C12Q1/48G01N33/68C07D311/18C07D311/82C07D473/32
    • C12Q1/37C07D311/18C07D311/82C07D473/32C12Q1/48G01N33/6875G01N2500/00Y02P20/55
    • Provided are a method for measuring histone methyltransferase activity, a method for screening for compounds that inhibit histone methyltransferase activity, a reagent kit for measuring histone methyltransferase activity, and a kit for screening for compounds that inhibit histone methyltransferase activity. A substrate compound represented by general formula (I): R1-X-K-R2 (I), or a salt thereof, wherein R1 represents a hydrogen atom or a protecting group for an amino terminus; X represents a peptide consisting of 0 or 1 or more amino acid residues; K represents a lysine residue; and R2 represents a dye label linked via an amide bond to the carbonyl terminus of a lysine residue, wherein the cleavage of the amide bond by peptidase changes the fluorescence property or chromogenic property of the dye label, and the methylation of the ε amino group of the lysine residue by the histone methyltransferase decreases susceptibility to peptidase, is used.
    • 提供了测定组蛋白甲基转移酶活性的方法,用于筛选抑制组蛋白甲基转移酶活性的化合物的方法,用于测定组蛋白甲基转移酶活性的试剂盒和用于筛选抑制组蛋白甲基转移酶活性的化合物的试剂盒。 由通式(I)表示的底物化合物:R1-X-K-R2(I)或其盐,其中R1表示氢原子或氨基末端的保护基; X表示由0或1个或更多个氨基酸残基组成的肽; K表示赖氨酸残基; R2表示通过酰胺键与赖氨酸残基的羰基末端连接的染料标记,其中通过肽酶切割酰胺键改变染料标记的荧光性质或显色性质,以及染料标记的甲基化。 使用组蛋白甲基转移酶的赖氨酸残基的氨基降低对肽酶的易感性。