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Target specific screens and their use for discovering small organic molecular pharmacophores

机译:靶向特定的筛选及其在发现有机小分子药效团中的用途

摘要

The invention relates to a general process by which recombinantly derived variable domains of antibodies encompassing either or both light and heavy variable regions with or without respective constant regions are engineered and selected for identification of unique surface domains of pharmaceutical targets or parts thereof which regulate target function. The recombinant antibodies are useful as reagents for high volume, rapid screening of occupation of the active surface domains by natural or synthetic entities. This invention is also directed to elucidating the three-dimensional conformation of the antibodies, or parts thereof, which bind to the pharmaceutical targets and confers activity. Methods for creating high resolution molecular models which can direct the synthesis of biologically active small organic molecules useful as viable discovery drug leads are also provided.
机译:本发明涉及一种通用方法,通过该通用方法,工程改造并选择涵盖具有轻或重可变区的抗体的重组衍生可变区,所述轻或重可变区具有或不具有各自的恒定区,以鉴定调节靶标功能的药物靶标或其部分的独特表面结构域。重组抗体可用作试剂,用于大量,快速筛选天然或合成实体对活性表面结构域的占用。本发明还涉及阐明结合药物靶标并赋予活性的抗体或其部分的三维构象。还提供了用于创建高分辨率分子模型的方法,该模型可以指导用作活的发现药物前导物的生物活性小有机分子的合成。

著录项

  • 公开/公告号EP1028315A3

    专利类型

  • 公开/公告日2004-01-02

    原文格式PDF

  • 申请/专利权人 DGI BIOTECHNOLOGIES INC.;

    申请/专利号EP20000111315

  • 发明设计人 BLUME ARTHUR J.;

    申请日1995-08-02

  • 分类号G01N33/53;G01N33/554;G01N33/58;G01N33/68;C07K16/44;C07K19/00;C12N15/13;

  • 国家 EP

  • 入库时间 2022-08-21 22:57:16

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