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NMR 研究揭示 hERG K+ 通道结构与功能。

Insights into hERG K+ channel structure and function from NMR studies.

机构信息

Mark Cowley Lidwill Research Programme in Cardiac Electrophysiology, Molecular Cardiology and Biophysics Division, Victor Chang Cardiac Research Institute, 405 Liverpool Street, Darlinghurst, NSW, 2010, Australia.

出版信息

Eur Biophys J. 2013 Jan;42(1):71-9. doi: 10.1007/s00249-012-0808-6. Epub 2012 May 3.

Abstract

The unique gating kinetics of hERG K(+) channels are critical for normal cardiac repolarization, and patients with mutations in hERG have a markedly increased risk of cardiac arrhythmias and sudden cardiac arrest. HERG K(+) channels are also remarkably promiscuous with respect to drug binding, which has been a very significant problem for the pharmaceutical industry. Here, we review the progress that has been made in understanding the structure and function of hERG K(+) channels with a particular focus on nuclear magnetic resonance studies of the domains of the hERG K(+) channel.

摘要

hERG K(+) 通道独特的门控动力学对于正常的心脏复极化至关重要,而 hERG 突变的患者发生心脏心律失常和心搏骤停的风险显著增加。HERG K(+) 通道对药物结合也非常混杂,这对制药行业来说是一个非常严重的问题。在这里,我们回顾了在理解 hERG K(+) 通道的结构和功能方面所取得的进展,特别关注 hERG K(+) 通道结构域的核磁共振研究。

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