A high-throughput HERG potassium channel function assay: An old assay with a new look
A high-throughput HERG potassium channel function assay: An old assay with a new look
复制标题
DOI：
10.1081/ddc-120002451
复制
发表时间：
2002-01-01
影响因子：
3.4
通讯作者：
Yu, WF
中科院分区：
文献类型：
--
作者：
Cheng, CS;Alderman, D;Yu, WF
在本文中，我们描述了一种使用放射性铷 (Rb-86) 流出物以高通量筛选 (HTS) 形式筛选功能性人醚 - go-go 相关基因 (HERD) K+ 通道的测定方法。该测定提供了另一种方法来检查化合物和 HERG K+ 通道之间的功能相互作用。进行了后续实验和讨论，以解决影响 Rb 流出测定中效力评估的各种因素。详细讨论了可能影响测定结果的因素，例如测定时间、流出速率和化合物阻断动力学。我们的结果为测定结果的差异提供了一些解释，并为在制药行业中使用 Rb 流出测定来评估化合物与 HERG K+ 通道的相互作用提供了一些指导。
In this paper, we describe an assay using radioactive rubidium (Rb-86) efflux to screen functional human ether-a go-go-related gene (HERD) K+ channels in a high-throughput screening (HTS) format. This assay offers an alternative way to examine functional interactions between chemical compounds and HERG K+ channels. Follow-up experiments and discussions were carried out to address a variety of factors that affect potency evaluation within the Rb efflux assay. Factors that can affect the assay results, such as assay time, efflux rate, and compound blocking kinetics, are discussed in detail. Our results provide some explanations for the variances of the assay results and offer some guidelines for using the Rb efflux assay to evaluate compound interactions with HERG K+ channels in the pharmaceutical industry.