BPR-3P0128抑制肠道病毒71的RNA依赖性RNA聚合酶延伸和VPg尿苷酰化活性。
BPR-3P0128 inhibits RNA-dependent RNA polymerase elongation and VPg uridylylation activities of Enterovirus 71.
作者信息
Velu Arul Balaji, Chen Guang-Wu, Hsieh Po-Ting, Horng Jim-Tong, Hsu John Tsu-An, Hsieh Hsing-Pang, Chen Tzu-Chun, Weng Kuo-Feng, Shih Shin-Ru
机构信息
Graduate Institute of Biomedical Sciences, College of Medicine, Chang Gung University, Taoyuan, Taiwan; Research Center for Emerging Viral Infections, College of Medicine, Chang Gung University, Taoyuan, Taiwan.
Research Center for Emerging Viral Infections, College of Medicine, Chang Gung University, Taoyuan, Taiwan; Department of Computer Science and Information Engineering, College of Medicine, Chang Gung University, Taoyuan, Taiwan.
出版信息
Antiviral Res. 2014 Dec;112:18-25. doi: 10.1016/j.antiviral.2014.10.003. Epub 2014 Oct 18.
Enterovirus 71 (EV71) infections can cause hand, foot, and mouth disease with severe neurological complications. Because no clinical drug is available for treating EV71 infections, developing an efficient antiviral medication against EV71 infection is crucial. This study indicated that 6-bromo-2-[1-(2,5-dimethylphenyl)-5-methyl-1H-pyrazol-4-yl] quinoline-4-carboxylic acid (BPR-3P0128) exhibits excellent antiviral activity against EV71 (EC50 = 0.0029 μM). BPR-3P0128 inhibits viral replication during the early post infection stage, targets EV71 RNA-dependent RNA polymerase and VPg uridylylation, and also reduces viral RNA accumulation levels and inhibits viral replication of EV71.
肠道病毒71型（EV71）感染可引发手足口病并伴有严重的神经并发症。由于目前尚无临床药物可用于治疗EV71感染，因此开发一种有效的抗EV71感染抗病毒药物至关重要。本研究表明，6-溴-2-[1-(2,5-二甲基苯基)-5-甲基-1H-吡唑-4-基]喹啉-4-羧酸（BPR-3P0128）对EV71表现出优异的抗病毒活性（半数有效浓度EC50 = 0.0029 μM）。BPR-3P0128在感染后早期阶段抑制病毒复制，作用于EV71的RNA依赖性RNA聚合酶和VPg尿苷化，还可降低病毒RNA积累水平并抑制EV71的病毒复制。
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