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Current Medicinal Chemistry

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ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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Review Article

How to Fluorescently Label the Potassium Channel: A Case in hERG

Author(s): Xiaomeng Zhang, Beilei Wang, Zhenzhen Liu, Yubin Zhou and Lupei Du*

Volume 27, Issue 18, 2020

Page: [3046 - 3054] Pages: 9

DOI: 10.2174/0929867326666181129094455

Price: $65

Abstract

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.

Keywords: hERG channel, small molecule fluorescent probe, turn-on switch, fluorophore, recognition motif, Cryo- EM structure.

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