Zhang Xiaomeng, Liu Tingting, Wang Beilei, Gao Yuqi, Liu Pan, Li Minyong, Du Lupei
Department of Medicinal Chemistry , Key Laboratory of Chemical Biology (MOE) , School of Pharmacy , Shandong University , Jinan , Shandong 250012 , China . Email:
Medchemcomm. 2019 Feb 26;10(4):513-516. doi: 10.1039/c8md00562a. eCollection 2019 Apr 1.
Based on the scaffold of astemizole, three novel turn-on fluorescent probes (-) for human ether-a-go-go-related gene (hERG) potassium channel were developed herein. These probes have reasonable fluorescence properties, acceptable cell toxicity, and potent inhibitory activity, all of which contribute to cell imaging at the nanomolar level. Overall, these probes have the potential for setting up a screening system for hERG channels.
基于阿司咪唑的骨架,本文开发了三种新型的用于人醚 - 去极化相关基因(hERG)钾通道的开启型荧光探针(-)。这些探针具有合理的荧光特性、可接受的细胞毒性和有效的抑制活性,所有这些都有助于在纳摩尔水平上进行细胞成像。总体而言,这些探针具有建立hERG通道筛选系统的潜力。