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1. 发明授权

US07081360B2 Expression of G protein-coupled receptors with altered ligand binding and/or coupling properties 失效
标题翻译：具有改变的配体结合和/或偶联性质的G蛋白偶联受体的表达
公开(公告)号：US07081360B2
公开(公告)日：2006-07-25
申请号：US09362286
申请日：1999-07-27
申请人： Anupama K. Nadkarni , Joshua Trueheart
发明人： Anupama K. Nadkarni , Joshua Trueheart
IPC分类号： C12N1/19 , C07K14/705
CPC分类号： C07K14/705 , A61K38/00
摘要： Modified forms of G protein-coupled receptors which display altered ligand binding and/or coupling properties are provided as well as cells expressing such receptors and assays utilizing these cells for screening and identifying pharmaceutically effective compounds that specifically modulate the activity of a these modified forms of G protein coupled receptors. Yeast or mammalian cells can be used to express such receptors. The subject assays enable rapid screening of large numbers of compounds (e.g., compounds in a library) to identify those which are receptor agonists or antagonists. Compositions of matter, such as these novel receptors, novel recombinant yeast cells and novel gene constructs, are also provided. The instant assays provide a convenient format for discovering compounds which can be useful in modulating cellular function, as well as in understanding the pharmacology of compounds that specifically interact with these modified forms G protein coupled receptors.
摘要翻译：提供显示改变的配体结合和/或偶联性质的G蛋白偶联受体的修饰形式以及表达这些受体的细胞和利用这些细胞的测定法用于筛选和鉴定特异性调节这些修饰形式的活性的药学上有效的化合物 G蛋白偶联受体。酵母或哺乳动物细胞可用于表达此类受体。本发明的分析使得能够快速筛选大量化合物（例如文库中的化合物），以鉴定那些是受体激动剂或拮抗剂的化合物。还提供了诸如这些新型受体的物质组合，新型重组酵母细胞和新型基因构建体。本发明提供了发现可用于调节细胞功能的化合物以及理解与这些修饰形式G蛋白偶联受体特异性相互作用的化合物的药理学的方便的形式。

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