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1. 发明申请

US20060035280A1 Screening methods for inhibitors of protein-protein binding interactions 审中-公开
标题翻译：蛋白质 - 蛋白质结合相互作用抑制剂的筛选方法
公开(公告)号：US20060035280A1
公开(公告)日：2006-02-16
申请号：US11034312
申请日：2005-01-12
申请人： Kuo-Sen Huang , Lyubomir Vassilev
发明人： Kuo-Sen Huang , Lyubomir Vassilev
IPC分类号： G01N33/53
CPC分类号： G01N33/582 , G01N2333/4704 , G01N2500/02
摘要： Protein-protein interactions represent a large and important group of drug targets involved in the development and progression of human diseases. However, their utilization in drug discovery has been hampered by the low probability of identifying small-molecule inhibitors able to disrupt protein binding with desirable potency and selectivity. Therefore, the capability for rapid screening of large compound libraries has been critical for the exploration of this target class. The present invention relates to a homogeneous time-resolved fluorescence assay for identification of inhibitors of Cks1-Skp2 binding that plays a critical role in the ubiquitin-dependent degradation of p27. The assay was implemented in a 1536-well format using the new Zeiss uHTS robot and achieved a throughput in excess of 100,000 data points per day. A protocol for a fully automated high throughput IC50 determination was developed for hit validation. The basic 1536 well screening platform reported here is simple, robust and cost effective. It is widely applicable to any protein-protein interaction of therapeutic interest.
摘要翻译：蛋白质 - 蛋白质的相互作用代表着涉及人类疾病发展和进展的大量重要的药物靶点。然而，它们在药物发现中的利用受到了鉴定能够以期望的效力和选择性破坏蛋白质结合的小分子抑制剂的可能性低的障碍。因此，快速筛选大型化合物库的能力对于探索这一目标阶段至关重要。本发明涉及用于鉴定在p27的泛素依赖性降解中起重要作用的Cks1-Skp2结合抑制剂的均匀时间分辨荧光测定法。该测定使用新的Zeiss uHTS机器人以1536孔格式实现，并且每天达到超过100,000个数据点的吞吐量。开发了用于命中验证的全自动高通量IC 50确定的协议。这里报道的基本的1536井筛选平台是简单，健壮和具有成本效益的。它广泛适用于治疗兴趣的任何蛋白质 - 蛋白质相互作用。

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