Current Medicinal Chemistry ( IF 3.5 ) Pub Date : 2020-05-31 , DOI: 10.2174/0929867326666181129094455 Xiaomeng Zhang 1 , Beilei Wang 1 , Zhenzhen Liu 1 , Yubin Zhou 2 , Lupei Du 1
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.
中文翻译:
如何对钾通道进行荧光标记:以hERG为例。
hERG(人类与神经元相关的基因)钾通道在心脏动作电位复极化中起重要作用,是遗传性和药物诱发的长QT综合征的原因。最近,确定了捕获hERG通道开放构象的Cryo-EM结构,从而推动了对3.8Å分辨率的hERG通道的研究。该报告主要集中在总结针对hERG通道的几种荧光探针的设计原理和应用,这可以动态实时监测钾孔通道亲和力,从而进一步增进对通道的了解。