Pharmacological corrections of the mutant hERG channels by posaconazole

Luo Chaodi; Zheng Xinglong; Li Jing; Zhang Yongjian; Shi Tao; Yan Yang; Han Dan

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Pharmacological corrections of the mutant hERG channels by posaconazole

机译：posaconazole突变疱疹频道的药理校正

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Properties of mutant human ether-a-go-go-related gene (hERG) channels can be modified by some antibiotics. However, the pharmacological effects of posaconazole on cardiomyocyte hERG channels remain unclear. Whole-cell patch clamping, western blotting and laser confocal scanning microscopy were used to evaluate the effects of posaconazole on wild-type (WT)-, A561V- and L539 fs/47-hERG channels expressed in human embryonic kidney (HEK) 293 cells. In electrophysiological experiments, HEK 293 cells were transiently co-transfected with equal amounts of WT-hERG, WT+A561 V-hERG and WT+L539 fs/47-hERG plasmids to mimic a heterozygous genotype. Posaconazole (30 mu M) increased tail currents in cells expressing WT-hERG, WT+A561 V-hERG and WT+L539 fs/47-hERG by 82.65%, 147.72% and 134.73%, respectively, compared to controls. Posaconazole increased hERG protein expression in cells expressing WT-hERG, WT+A561 V-hERG and WT+L539 fs/47-hERG compared to controls condition as well as their trafficking to the cell membrane. To our knowledge, this is the first study to show that antifungal agent posaconazole rescues the mutant A561 V-hERG and L539 fs/47-hERG channels by altering the gating kinetics, enhancing the expression and trafficking of hERG channels. The results demonstrate that posaconazole could be a promising candidate for the prevention and treatment of long QT syndrome and other arrhythmia-related diseases.

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来源
《Clinical and experimental pharmacology & physiology》 |2021年第6期|共14页
作者
Luo Chaodi; Zheng Xinglong; Li Jing; Zhang Yongjian; Shi Tao; Yan Yang; Han Dan;
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作者单位

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiol Xian Peoples R China;

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiovasc Surg 277 Yanta West Rd Xian 710061;

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiovasc Surg 277 Yanta West Rd Xian 710061;

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiovasc Surg 277 Yanta West Rd Xian 710061;

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiovasc Surg 277 Yanta West Rd Xian 710061;

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiovasc Surg 277 Yanta West Rd Xian 710061;

Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Cardiovasc Surg 277 Yanta West Rd Xian 710061;

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原文格式 PDF
正文语种 eng
中图分类药理学;
关键词
A561 V; anti-arrhythmia; hERG; L539 fs/47; LQT2; posaconazole;

机译：A561 V;抗心律失常;HERG;L539 FS / 47;LQT2;Posaconazole;

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专利

1. The protease inhibitor atazanavir blocks hERG K+ channels expressed in HEK293 cells and obstructs hERG protein transport to cell membrane [J] . Sheng-na HAN, Xiao-yan SUN, Zhao ZHANG, 中国药理学报：英文版 . 2015,第004期
2. Comparison of the effects of DC031050,a class Ⅲ antiarrhythmic agent, on hERG channel and three neuronal potassium channels [J] . Ping LI, Hai-feng SUN, Ping-zheng ZHOU, 中国药理学报：英文版 . 2012,第006期
3. Construction of a HERG mutant L539fs/47-*558W pEGFP vector and the expression of the fusion protein in HEK293 cells [J] . ZHANG Junbo, Lü Ying, ZHANG Aifeng, 中国人民解放军军医大学学报（英文版） . 2013,第004期
4. Recognition of high-specificity hERG K+channel inhibitor-induced arrhythmia in cardiomyocytes by automated template matching [J] . Hao Wang, Ning Hu, Hongbo Li, 微系统与纳米工程（英文） . 2021,第002期
5. Translational toxicology and rescue strategies of the hERG channel dysfunction: biochemical and molecular mechanistic aspects [J] . Kai-ping ZHANG, Bao-feng YANG, Bao-xin LI 中国药理学报：英文版 . 2014,第012期
6. Mutant hERG channel traffic jam. Focus on "Pharmacological correction of long QT-linked mutations in KCNH2 (hERG) increases the trafficking of Kv11.1 channels stored in the transitional endoplasmic reticulum" [J] . Ramon J. Ayon, Ruby A. Fernez, Jason X.-J. Yuan American Journal of Physiology . 2013,第5Pta1期

机译：突变疱疹渠道交通堵塞。专注于“Long Qt-Linked突变在KCNH2（HERG）中的药理校正增加了储存在过渡内质网中的KV11.1通道的贩运”
7. Pharmacological rescue of trafficking defective HERG channels formed by coassembly of wild-type and long QT mutant N470D subunits. [J] . Gong Q, Anderson CL, January CT, American Journal of Physiology . 2004,第2期

机译：通过野生型和长QT突变体N470D亚基的共同装配形成的贩运有缺陷的HERG通道的药理抢救。
8. Pharmacological correction of long QT-linked mutations in KCNH2 (hERG) increases the trafficking of Kv11.1 channels stored in the transitional endoplasmic reticulum [J] . Smith JL, Reloj AR, Nataraj PS, American Journal of Physiology . 2013,第5Pta1期

机译：KCNH2（HERG）中长QT连接突变的药理校正增加了储存在过渡内质网中的KV11.1通道的贩运
9. Quantification of hERG potassium channel block from the ECG [C] . Johan de Bie, W. Brian Chiu, David W. Mortara, Computing in Cardiology Conference . 2017

机译：从心电图中定量HERG钾通道块
10. Computational pharmacology of the hERG potassium channel. [D] . Babcock, Joseph James. 2013

机译：hERG钾通道的计算药理学。
11. Mechanisms of pharmacological rescue of trafficking defective hERG mutant channels in human long QT syndrome [O] . Qiuming Gong, Melanie A. Jones, Zhengfeng Zhou -1

机译：长期QT综合征贩运缺陷性hERG突变通道的药理挽救机制。
12. hERG Trafficking and Pharmacological Rescue of LQTS-2 Mutant Channels [O] . S. Kass, Colleen E. Clancy, G. A. Robertson, 2015

机译：hERG贩运和药物拯救LQTs-2突变通道
13. Effects of Pharmacologic and Genetic Inhibition of Alk on Cognitive Impairments in NF1 Mutant Mice. [R] . Raber, J., Weiss, J., Weber, S. 2016

机译：药理学和遗传抑制对NF1突变小鼠认知障碍的影响。

Pharmacological corrections of the mutant hERG channels by posaconazole

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