Method for identifying compounds of therapeutic interest

    公开(公告)号:US10048253B2

    公开(公告)日:2018-08-14

    申请号:US14409424

    申请日:2013-06-28

    申请人: UCB PHARMA S.A.

    摘要: The present invention relates to an improved method for drug discovery. In particular the present invention provides a method of identifying compounds capable of binding to a functional conformational state of a protein of interest or protein fragment thereof, said method comprising the steps of: (a) Binding a function-modifying antibody to the target protein of interest or a fragment thereof to provide an antibody-constrained protein or fragment, wherein the antibody has binding kinetics with the protein or fragment which are such that it has a low dissociation rate constant, (b) Providing a test compound which has a low molecular weight, (c) Evaluating whether the test compound of step b) binds the antibody constrained protein or fragment, and (d) Select a compound from step c) based on the ability to bind to the protein or fragment thereof.

    Method for Identifying Compounds of Therapeutic Interest
    6.
    发明申请
    Method for Identifying Compounds of Therapeutic Interest 审中-公开
    识别治疗兴趣化合物的方法

    公开(公告)号:US20150219635A1

    公开(公告)日:2015-08-06

    申请号:US14409424

    申请日:2013-06-28

    申请人: UCB PHARMA S.A.

    IPC分类号: G01N33/53 G06F19/16

    摘要: The present invention relates to an improved method for drug discovery. In particular the present invention provides a method of identifying compounds capable of binding to a functional conformational state of a protein of interest or protein fragment thereof, said method comprising the steps of: (a) Binding a function-modifying antibody to the target protein of interest or a fragment thereof to provide an antibody-constrained protein or fragment, wherein the antibody has binding kinetics with the protein or fragment which are such that it has a low dissociation rate constant, (b) Providing a test compound which has a low molecular weight, (c) Evaluating whether the test compound of step b) binds the antibody constrained protein or fragment, and (d) Select a compound from step c) based on the ability to bind to the protein or fragment thereof.

    摘要翻译: 本发明涉及药物发现的改进方法。 特别地,本发明提供了鉴定能够结合目标蛋白质或其蛋白质片段的功能构象状态的化合物的方法,所述方法包括以下步骤:(a)将功能修饰抗体与靶蛋白的结合 提供抗体约束蛋白或片段,其中抗体与蛋白质或片段具有结合动力学,使得其具有低解离速率常数,(b)提供具有低分子量的测试化合物 (c)评估步骤b)的测试化合物是否结合抗体约束蛋白或片段,和(d)基于与蛋白质或其片段结合的能力从步骤c)中选择化合物。