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1.发明申请METHOD FOR DETECTING COMPOUNDS MODULATING DIMERS OF VFT DOMAIN MEMBRANE PROTEINS 有权检测化合物调节VFT域膜蛋白二聚体的方法公开(公告)号：US20120115176A1
公开(公告)日：2012-05-10
申请号：US13266222
申请日：2010-04-29
CPC分类号： G01N33/542 , G01N33/9426 , G01N2333/726 , G01N2500/04
摘要： The invention relates to a method for selecting compounds having a modulating effect on the activation state of a dimer of VFT-domain proteins expressed in cell membranes present in a measuring medium, said dimer consisting of a first protein and of a second protein, said proteins being identical or different, wherein this method comprises the following steps: (a) labeling the first and second proteins in the N-terminal portion of their VFT domains with the members of a pair of FRET partners, the Förster radius (R0) of said pair being between 20 and 55 Å; (b) measuring the FRET signal in the absence and in the presence of the test compound within a predetermined time window; (c) selecting the test compound as a modulating compound if a difference in FRET signal in the absence and in the presence of test compound is measured in step (b). The invention can be used in the search for new medicaments and new taste modulators.
摘要翻译： 本发明涉及一种选择对存在于测量介质中的细胞膜中表达的VFT结构域蛋白的二聚体的活化状态具有调节作用的化合物的方法，所述二聚体由第一种蛋白质和第二种蛋白质组成，所述蛋白质 相同或不同，其中该方法包括以下步骤：（a）用一对FRET伴侣的成员将其VFT结构域的N末端部分中的第一和第二蛋白质标记，所述第一和第二蛋白质的所述F 对在20和55之间; （b）在预定时间窗内测试化合物不存在和存在时测量FRET信号; （c）如果在步骤（b）中测定了在不存在和存在测试化合物的情况下FRET信号的差异，则选择测试化合物作为调节化合物。 本发明可用于寻找新的药物和新的调味剂。
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2.发明授权Method for detecting compounds modulating dimers of VFT domain membrane proteins 有权检测调节VFT结构域膜蛋白二聚体的化合物的方法公开(公告)号：US08697380B2
公开(公告)日：2014-04-15
申请号：US13266222
申请日：2010-04-29
CPC分类号： G01N33/542 , G01N33/9426 , G01N2333/726 , G01N2500/04
摘要： The invention relates to a method for selecting compounds having a modulating effect on the activation state of a dimer of VFT-domain proteins expressed in cell membranes present in a measuring medium, said dimer consisting of a first protein and of a second protein, said proteins being identical or different, wherein this method comprises the following steps: (a) labeling the first and second proteins in the N-terminal portion of their VFT domains with the members of a pair of FRET partners, the Förster radius (R0) of said pair being between 20 and 55 Å; (b) measuring the FRET signal in the absence and in the presence of the test compound within a predetermined time window; (c) selecting the test compound as a modulating compound if a difference in FRET signal in the absence and in the presence of test compound is measured in step (b). The invention can be used in the search for new medicaments and new taste modulators.
摘要翻译： 本发明涉及一种选择对存在于测量介质中的细胞膜中表达的VFT结构域蛋白的二聚体的活化状态具有调节作用的化合物的方法，所述二聚体由第一种蛋白质和第二种蛋白质组成，所述蛋白质 相同或不同，其中该方法包括以下步骤：（a）用一对FRET伴侣的成员将其VFT结构域的N末端部分中的第一和第二蛋白质标记，所述第一和第二蛋白质的所述F 对在20和55之间; （b）在预定时间窗内测试化合物不存在和存在时测量FRET信号; （c）如果在步骤（b）中测定了在不存在和存在测试化合物的情况下FRET信号的差异，则选择测试化合物作为调节化合物。 本发明可用于寻找新的药物和新的调味剂。
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