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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 protein (NS5A) is a new target for the treatment of hepatitis C virus infection. Although NS5A protein does not possess enzymatic activity, it plays an important role in viral RNA replication. Small molecule inhibitors of the NS5A protein show strong inhibitory activity against virus growth in vitro and preliminary clinical evaluation also confirmed that the NS5A inhibitor inhibits the growth of the hepatitis C virus in vivo. Therefore, the development of efficient NS5A small molecule inhibitors provides a new strategy for the treatment of hepatitis C. This review summarizes the structural types, structure-activity relationship, biological activity and mechanism of action of NS5A inhibitors.