基于细胞的 hERG 通道抑制assay 在高通量格式中。
Cell-Based hERG Channel Inhibition Assay in High-Throughput Format.
机构信息
National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD, USA.
出版信息
Methods Mol Biol. 2022;2474:21-28. doi: 10.1007/978-1-0716-2213-1_3.
Abstract
Human ether-a-go-go-related gene (hERG) channel plays an essential role in the repolarization of the cardiac action potential. Genetic mutations and some chemicals/drugs interfere with hERG channel activity, which may prolong the QT interval and potentially cause long QT syndrome. The FluxOR™ thallium flux assay performed in two cell lines, U2OS and HEK293, with stable hERG expression can be used to identify compounds that inhibit hERG channel activity. This chapter describes a cell-based hERG channel inhibition assay that has been optimized and performed in a 1536-well plate format. The homogeneous and robust assay can be used to identify compounds that inhibit hERG channel activity.
摘要
人类 ether-a-go-go 相关基因 (hERG) 通道在心脏动作电位复极化中发挥着重要作用。遗传突变和一些化学物质/药物会干扰 hERG 通道的活性，从而延长 QT 间期，并可能导致长 QT 综合征。在稳定表达 hERG 的 U2OS 和 HEK293 两种细胞系中进行的 FluxOR™ 铊通量测定可用于鉴定抑制 hERG 通道活性的化合物。本章描述了一种基于细胞的 hERG 通道抑制测定法，该方法已在 1536 孔板格式中进行了优化和实施。这种均相且稳健的测定法可用于鉴定抑制 hERG 通道活性的化合物。
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