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2. 发明申请

WO1996040721A1 A CYTOTOXICITY-BASED GENETIC SELECTION SYSTEM (TOXSEL) 审中-公开
标题翻译：基于细胞毒性的遗传选择系统（TOXSEL）
公开(公告)号：WO1996040721A1
公开(公告)日：1996-12-19
申请号：PCT/US1996008356
申请日：1996-06-03
申请人： EMORY UNIVERSITY , PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： EMORY UNIVERSITY , PRESIDENT AND FELLOWS OF HARVARD COLLEGE , FU, Haian , COLLIER, R., John , DINGLEDINE, Raymond
IPC分类号： C07H21/04
CPC分类号： C12Q1/6897 , C12N15/1055 , G01N33/5014 , G01N2500/00
摘要： The invention provides a cytotoxicity-based genetic selection (TOXSEL) method and related testing kit for the identification and positive selection of molecules or mutations that are capable of disrupting a specific protein-protein interaction. The invention enables positive selection of molecules disruptive of specific protein-protein interactions by virtue of the presence in the TOXSEL system of a toxin reporter gene. A disrupted protein-protein interaction precludes expression of the toxin reporter gene and, consequently, allows survival of the host cell. TOXSEL technology enables large-scale screening for drugs or small molecules capable of disrupting specific protein-protein interactions critical in processes such as cellular signalling, carcinogenesis, etc. The positive selection of molecules or mutations capable of interfering with specific protein-protein interactions permits the identification of amino acid residues or motifs critical in the protein-protein interactions and permits the design of drugs for therapeutic or diagnostic applications.
摘要翻译：本发明提供基于细胞毒性的遗传选择（TOXSEL）方法和用于鉴定和阳性选择能够破坏特定蛋白质 - 蛋白质相互作用的分子或突变的相关检测试剂盒。本发明通过在毒素报告基因的TOXSEL系统中的存在能够正确选择破坏特定蛋白质 - 蛋白质相互作用的分子。破坏的蛋白质 - 蛋白质相互作用排除了毒素报告基因的表达，因此允许宿主细胞的存活。 TOXSEL技术可以大规模筛选能够破坏细胞信号传导，致癌作用等过程中特定蛋白质 - 蛋白质相互作用关键的药物或小分子。能够干扰特定蛋白质 - 蛋白质相互作用的分子或突变的阳性选择允许识别蛋白质 - 蛋白质相互作用中关键的氨基酸残基或基序，并允许药物设计用于治疗或诊断应用。

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