CAS Key Laboratory of Molecular Virology and Immunology, Unit of Viral Hepatitis, Institut Pasteur of Shanghai, Chinese Academy of Sciences, Shanghai, 200031, China; Shanghai Tech University, Shanghai, 201210, China; University of Chinese Academy of Sciences, Beijing, 100049, China.
Department of Infectious Disease, Ruijin Hospital, Shanghai Jiaotong University School of Medicine, Shanghai, China.
Antiviral Res. 2019 Nov;171:104612. doi: 10.1016/j.antiviral.2019.104612. Epub 2019 Sep 19.
Hepatitis C virus (HCV), a major causative agent of chronic hepatitis, is a positive-stranded RNA virus and has a high degree of genetic diversity due to its error-prone RNA-dependent RNA polymerase. Development of direct-acting antiviral agents (DAAs) has greatly improved the therapeutic outcome of chronic hepatitis C patients. However, naturally existing resistance-associated variants (RAVs) or occurrence of resistance-associated substitutions (RASs) in the HCV genome may impose a challenge to the long-term success of the DAA-based therapies. Genotype-3 HCV is the most difficult genotype to treat by DAAs, but the underlying molecular mechanisms remain to be explored. Here we developed a novel genotype-3a subgenomic replicon PR87A7 by screening a HCV cDNA pool amplified from a patient serum RNA. PR87A7 replicon displayed strong resistance to anti-NS3 DAAs, mainly owing to a genotype-3-specific polymorphism 168Q in NS3. Introduction of NS3 168Q into a genotype-2a JFH1 strain rendered resistance to anti-NS3 DAAs while greatly diminished the viral replication, and yet this fitness defect can be rescued by additional genotype-3-specific polymorphism. In conclusion, we developed a novel genotype-3a subgenomic replicon by a functional screening approach, and revealed genotype-3-specfic amino acid residues that confer resistance to anti-NS3 DAAs while retaining viral fitness.
丙型肝炎病毒(HCV)是慢性肝炎的主要致病因子,是一种正链 RNA 病毒,由于其易错的 RNA 依赖性 RNA 聚合酶,具有高度的遗传多样性。直接作用抗病毒药物(DAAs)的开发极大地改善了慢性丙型肝炎患者的治疗效果。然而,HCV 基因组中天然存在的耐药相关变异(RAVs)或耐药相关取代(RASs)可能对 DAA 为基础的治疗的长期成功构成挑战。基因型 3 HCV 是最难用 DAA 治疗的基因型,但潜在的分子机制仍有待探索。在这里,我们通过筛选从患者血清 RNA 扩增的 HCV cDNA 池,开发了一种新型基因型 3a 亚基因组复制子 PR87A7。PR87A7 复制子对抗 NS3 DAAs 表现出很强的耐药性,主要归因于 NS3 中的基因型 3 特异性多态性 168Q。将 NS3 168Q 引入基因型 2a JFH1 株系会导致对 NS3 DAAs 的耐药性,同时大大降低病毒复制能力,但这种适应性缺陷可以通过额外的基因型 3 特异性多态性得到挽救。总之,我们通过功能筛选方法开发了一种新型基因型 3a 亚基因组复制子,并揭示了赋予抗 NS3 DAAs 耐药性的基因型 3 特异性氨基酸残基,同时保留了病毒适应性。