标题:How to Fluorescently Label the Potassium Channel: A Case in hERG
作者:Zhang, Xiaomeng; Wang, Beilei; Liu, Zhenzhen; Zhou, Yubin; Du, Lupei
作者机构:[Zhang, Xiaomeng; Wang, Beilei; Liu, Zhenzhen; Du, Lupei] Shandong Univ, Sch Pharm, Key Lab Chem Biol MOE, Dept Med Chem, Jinan 250012, Shandong, Peop 更多
通讯作者:Du, L(dulupei@sdu.edu.cn)
通讯作者地址:Du, LP (corresponding author), Shandong Univ, Sch Pharm, Key Lab Chem Biol MOE, Dept Med Chem, Jinan 250012, Shandong, Peoples R China.
来源:CURRENT MEDICINAL CHEMISTRY
出版年:2020
卷:27
期:18
页码:3046-3054
DOI:10.2174/0929867326666181129094455
关键词:hERG channel; small molecule fluorescent probe; turn-on switch;; fluorophore; recognition motif; CryoEM structure
摘要: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 drug induced long QT syndrome. Recently, the Cryo-EM structure capturinv, the open conformation of hERG channel was determined, thus pushing the study on hERG channel at 3.8 A 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 understandinv, of the channels.
收录类别:SCOPUS;SCIE
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85086013578&doi=10.2174%2f0929867326666181129094455&partnerID=40&md5=eadc31aaa807e50b706c715bf238df97
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