如何对钾通道进行荧光标记：以 hERG 为例。
How to Fluorescently Label the Potassium Channel: A Case in hERG.
机构信息
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
Institute of Biosciences and Technology, College of Medicine, Texas A&M University, Houston, TX 77030, United States.
出版信息
Curr Med Chem. 2020;27(18):3046-3054. doi: 10.2174/0929867326666181129094455.
hERG (Human ether-a-go-go-related gene) potassium channel, which plays an essential role in cardiac action potential repolarization, is responsible for inherited and druginduced long QT syndrome. Recently, the Cryo-EM structure capturing the open conformation of hERG channel was determined, thus pushing the study on hERG channel at 3.8 Å resolution. This report focuses primarily on summarizing the design rationale and application of several fluorescent probes that target hERG channels, which enables dynamic and real-time monitoring of potassium pore channel affinity to further advance the understanding of the channels.
hERG（人 Ether-a-go-go 相关基因）钾通道在心脏动作电位复极化中起着至关重要的作用，是遗传性和药物诱导的长 QT 综合征的原因。最近，确定了 hERG 通道开放构象的冷冻电镜结构，从而将 hERG 通道的研究推进到 3.8Å分辨率。本报告主要侧重于总结几种靶向 hERG 通道的荧光探针的设计原理和应用，这些探针能够动态和实时监测钾通道亲和力，从而进一步加深对通道的理解。
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