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METHOD FOR MEASURING HISTONE DEACETYLASE ACTIVITY USING FLUORESCENT OR CHROMOPHORIC SUBSTRATE
METHOD FOR MEASURING HISTONE DEACETYLASE ACTIVITY USING FLUORESCENT OR CHROMOPHORIC SUBSTRATE
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机译:用荧光或色母体测定组蛋白去乙酰化活性的方法
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摘要
PROBLEM TO BE SOLVED: To provide a substrate for measuring histone deacetylase (HDAC) activity which enables a nonradioactive measurement of HDAC, identification of HDAC subtypes and also screening of inhibitors specific for respective subtypes, which has been considered to be impossible, and also to provide a method for measuring the enzymatic activity of HDAC and a method for screening the HDAC inhibitors using the substrate.;SOLUTION: A compound which contains a neighboring sequence of an acetylated part of histone H4, p53, or the like, and is represented by formula (I) (wherein, R1 is H or a protective group of an amino terminal; R2 is a group which is deacetylated by HDAC; R3 is a fluorescent or a chromophoric group which forms an amide bond between the carbonyl terminal of a lysine and changes its fluorescent or chromophoric characteristics in response to free amine generated from the hydrolysis of the amide bond; X is one or more amino acid residues; and (K) is a lysine residue) is used as the substrate for measuring the HDAC activity.;COPYRIGHT: (C)2003,JPO
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机译:解决的问题:提供一种用于测量组蛋白脱乙酰基酶(HDAC)活性的底物,该底物能够实现HDAC的非放射性测量,HDAC亚型的鉴定以及针对各个亚型的特异性抑制剂的筛选,这被认为是不可能的,并且提供一种测量HDAC酶活性的方法和一种使用底物筛选HDAC抑制剂的方法。解决方案:一种化合物,其包含组蛋白H4,p53等的乙酰化部分的相邻序列,并以式(I)(其中,R 1 Sub>是H或氨基末端的保护基; R 2 Sub>是被HDAC脱乙酰基的基团; R 3 Sub>是一个荧光或发色基团,它在赖氨酸的羰基末端之间形成一个酰胺键,并响应于酰胺键水解产生的游离胺而改变其荧光或发色特性; X是一个或多个氨基酸渣ues; (K)为赖氨酸残基)用作测量HDAC活性的底物。;版权:(C)2003,JPO
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