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