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    • 2. 发明授权
    • Screening for enzyme inhibitors
    • 筛选酶抑制剂
    • US06770451B2
    • 2004-08-03
    • US10137952
    • 2002-05-03
    • Riaz RouhaniInna Vainshtein
    • Riaz RouhaniInna Vainshtein
    • C12Q148
    • C07D498/22C12Q1/00C12Q1/34C12Q1/485G01N33/542G01N2500/02
    • Systems, including methods and reagents, for identifying enzyme inhibitors. The systems employ a conjugate of a known inhibitor of a target enzyme and an enzyme donor, an enzyme acceptor that binds to the enzyme donor to form an active indicator-enzyme complex, and a detectable substrate for the indicator enzyme. The assay is performed by combining the candidate agent, the conjugate of the known inhibitor and enzyme donor, the enzyme acceptor, and the substrate under binding conditions, where the candidate compound competes with the conjugate for the target enzyme. By measuring the rate of product formation or substrate depletion catalyzed by the indicator enzyme, the inhibitory activity of the candidate compound can be determined. The methodology is particularly applicable for target enzymes that have substrates or products that are difficult to synthesize and/or detect, such as kinases and phosphatases.
    • 用于鉴定酶抑制剂的系统,包括方法和试剂。 该系统使用已知的靶酶抑制剂和酶供体的缀合物,与酶供体结合以形成活性指示剂 - 酶复合物的酶受体和用于指示酶的可检测底物。 通过将候选试剂,已知抑制剂和酶供体的缀合物,酶受体和底物在结合条件下组合来进行测定,其中候选化合物与目标酶的缀合物竞争。 通过测量指示剂催化的产物形成或底物消耗的速率,可以测定候选化合物的抑制活性。 该方法特别适用于具有难以合成和/或检测的底物或产物的靶酶,例如激酶和磷酸酶。