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针对丙型肝炎病毒NS5B RNA依赖性RNA聚合酶的有前景疗法的发现与开发的最新进展。

Recent advances in discovery and development of promising therapeutics against hepatitis C virus NS5B RNA-dependent RNA polymerase.

作者信息

Wu Jim Zhen, Yao Nanhua, Walker Michelle, Hong Zhi

机构信息

Drug Discovery, Valeant Pharmaceutical International, 3300 Hyland Avenue, Costa Mesa, CA 92626, USA.

出版信息

Mini Rev Med Chem. 2005 Dec;5(12):1103-12. doi: 10.2174/138955705774933310.

Abstract

Lack of highly effective and safe therapeutics for hepatitis C virus (HCV) infection provides an opportunity as well as a challenge to discover novel and potent anti-HCV drugs. HCV NS5B RNA-dependent RNA polymerase (RdRp) is responsible for viral genome replication and thus constitutes a valid target for therapeutic intervention. To date, numerous HCV NS5B RdRp inhibitors have been discovered. This review focuses on the recent advances in discovery, mechanism of action studies and biological characterization of several distinct classes of potent inhibitors for NS5B RdRp. The clinical efficacy and developmental status of several promising compounds are also outlined.

摘要

缺乏针对丙型肝炎病毒(HCV)感染的高效且安全的治疗方法,这既带来了机遇,也带来了挑战,促使人们去发现新型强效抗HCV药物。HCV NS5B RNA依赖性RNA聚合酶(RdRp)负责病毒基因组复制,因此是治疗干预的有效靶点。迄今为止,已发现了众多HCV NS5B RdRp抑制剂。本综述聚焦于几类不同的强效NS5B RdRp抑制剂在发现、作用机制研究及生物学特性方面的最新进展。还概述了几种有前景的化合物的临床疗效及研发状况。

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