文章基本信息

标题：Novel cell-free high-throughput screening method for pharmacological tools targeting K+ channels
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作者：Zhenwei Su ; Emily C. Brown ; Weiwei Wang 等
期刊名称：Proceedings of the National Academy of Sciences
印刷版ISSN：0027-8424
电子版ISSN：1091-6490
出版年度：2016
卷号：113
期号：20
页码：5748-5753
DOI：10.1073/pnas.1602815113
语种：English
出版社：The National Academy of Sciences of the United States of America
摘要：K+ channels, a superfamily of ∼80 members, control cell excitability, ion homeostasis, and many forms of cell signaling. Their malfunctions cause numerous diseases including neuronal disorders, cardiac arrhythmia, diabetes, and asthma. Here we present a novel liposome flux assay (LFA) that is applicable to most K+ channels. It is robust, low cost, and high throughput. Using LFA, we performed small molecule screens on three different K+ channels and identified new activators and inhibitors for biological research on channel function and for medicinal development. We further engineered a hERG (human ether-à-go-go-related gene) channel, which, when used in LFA, provides a highly sensitive (zero false negatives on 50 hERG-sensitive drugs) and highly specific (zero false positives on 50 hERG-insensitive drugs), low-cost hERG safety assay.
关键词：liposome flux assay ; LFA ; K⁺ channel screening ; hERG safety assay