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

Author(s):

Xiaomeng Zhang, Beilei Wang, Zhenzhen Liu, Yubin Zhou and Lupei Du*   Pages 1 - 9 ( 9 )

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.

Affiliation:

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, Institute of Biosciences and Technology, College of Medicine, Texas A&M University, Houston, TX 77030, Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012



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