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Influenza A virus polymerase: an attractive target for next-generation anti-influenza therapeutics
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-01-12 , DOI: 10.1016/j.drudis.2018.01.028
Zhongxia Zhou , Tao Liu , Jian Zhang , Peng Zhan , Xinyong Liu

The influenza RNA-dependent RNA polymerase (RdRP) is conserved among different types of influenza virus, playing an important part in transcription and replication. In this regard, influenza RdRP is an attractive target for novel anti-influenza drug discovery. Herein, we will introduce the structural and functional information of influenza polymerase; and an overview of inhibitors targeting the PA endonuclease and PB2 cap-binding site is provided, along with the approaches utilized for identification of these inhibitors. The protein–protein interactions (PPIs) of the three polymerase subunits: PA, PB1 and PB2, are described based on the published crystal structures, and inhibitors targeting the PA–PB1 interaction are introduced briefly.



中文翻译:

甲型流感病毒聚合酶:下一代抗流感疗法的诱人靶标

依赖于流感RNA的RNA聚合酶(RdRP)在不同类型的流感病毒之间是保守的,在转录和复制中起着重要的作用。在这方面,RdRP流感是新型抗流感药物发现的有吸引力的靶标。在这里,我们将介绍流感聚合酶的结构和功能信息;并提供了针对PA核酸内切酶和PB2帽结合位点的抑制剂的概述,以及用于鉴定这些抑制剂的方法。基于已公开的晶体结构描述了三个聚合酶亚基:PA,PB1和PB2的蛋白质-蛋白质相互作用(PPI),并简要介绍了靶向PA-PB1相互作用的抑制剂。

更新日期:2018-01-12
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