丙型肝炎病毒非结构5A蛋白(NS5A)抑制剂研究进展  

Recent progress of non-structural 5A protein(NS5A) inhibitors as anti-hepatitis virus C agents

作　　者：王涛[1] 朱仕平[1] 张万年[1] 盛春泉[1] 

机构地区：[1]第二军医大学药学院,上海200433

出　　处：《中国药物化学杂志》2012年第6期533-539,共7页Chinese Journal of Medicinal Chemistry

基　　金：国家高技术研究发展计划项目(863项目;2012AA020302)

摘　　要：非结构5A蛋白(NS5A)是治疗丙型肝炎病毒感染的新靶标。尽管NS5A蛋白不具备酶催化活性,但它对病毒RNA复制起着重要作用。NS5A蛋白的小分子抑制剂显示出很强的体外抑制病毒生长的活性,并且初步的临床评价也证实了NS5A抑制剂能很好的抑制体内丙型肝炎病毒的生长。因此,研发高效的NS5A小分子抑制剂为治疗丙型肝炎提供了新的策略。本文综述了NS5A抑制剂的结构类型、构效关系、生物活性和作用机制等方面的研究进展。Non-structural 5A（NS5A） protein represents a new target for the treatment of infections caused by hepatitis virus C（HCV）. Although NS5A does not possess enzymatic activity, it plays an important role in viral RNA replication. Small molecules targeting NS5A have demonstrated profound antiviral effects. Mo- reover,related clinical proof-of-concept study with NS5A inhibitors have also shown good in vivo anti-HCV activity. Therefore,developing highly potent small molecule inhibitors of NS5A provides a new strategy for anti-HCV therapy. This review summarized recent progress of NS5A inhibitors including their chemotype, structure-activity relationships, biological activity and mode of action.

关 键 词：NS5A蛋白 抑制剂 丙型肝炎病毒 

分 类 号：R914[医药卫生—药物化学]