Why the study?
Following the determination of the open conformation Cryo-EM structure of the hERG channel at 3.8 Å resolution, dynamic and real-time monitoring tools were needed to further advance the understanding of the channels.
This review summarizes the design and application of fluorescent probes for real-time monitoring of hERG potassium channels, which are critical in cardiac repolarization and long QT syndrome.
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.
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Zhang et al. (2018) studied this question.
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