期刊
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
卷 113, 期 20, 页码 5748-5753出版社
NATL ACAD SCIENCES
DOI: 10.1073/pnas.1602815113
关键词
liposome flux assay; LFA; K+ channel screening; hERG safety assay
资金
- National Institutes of Health [GM43949]
- American Asthma Foundation
- Robertson Therapeutic Development Fund
- Bridge Fund
K+ channels, a superfamily of similar to 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-a-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.
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