Internal Medicine, IPC 424, Pfizer PGRD, Discovery Biology, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, United Kingdom.
Antimicrob Agents Chemother. 2011 Sep;55(9):4311-9. doi: 10.1128/AAC.00644-11. Epub 2011 Jun 27.
The current standard of care for hepatitis C virus (HCV) patients is cotreatment with human alpha interferon (IFN-α) and ribavirin. The host factor USP18 functions to regulate the interferon signaling pathway by acting as an off-switch. In order to understand whether the inhibition of USP18 represents a valid target for the enhancement of interferon treatment for chronic viral diseases, we have used a wide range of RNA interference (RNAi) reagents to suppress USP18 gene expression in Huh7 cell lines. We demonstrate that a USP18 knockdown results in IFN-α2a signaling (measured by increased IFN-stimulated response element [ISRE] reporter gene activity, 2',5'-oligoadenylate synthetase [2-5 OAS] expression, and ISG15 induction) that is increased by ∼100-fold, whereas the antiviral (AV) potency in both the Huh7 HCV subgenomic replicon assay and the Huh7.5 HCV infectious virus assay increased by ∼3-fold. While the degree of the USP18 knockdown of USP18 elicited by the different RNAi reagents correlated with the enhancement of IFN-α2a signaling, it did not correlate with the enhancement of AV activity. The failure of increased IFN-α2a signaling to fully translate into increased AV potency was also observed for encephalomyocarditis virus (EMCV) assays using Huh7.5 cells. These data suggest that the IFN-mediated AV response in Huh7.5 cells has only a limited dependence on USP18 activity.
目前丙型肝炎病毒(HCV)患者的标准治疗方法是联合使用人α干扰素(IFN-α)和利巴韦林。宿主因子 USP18 通过作为关闭开关来调节干扰素信号通路。为了了解抑制 USP18 是否代表增强慢性病毒疾病的干扰素治疗的有效靶点,我们使用了广泛的 RNA 干扰(RNAi)试剂来抑制 Huh7 细胞系中的 USP18 基因表达。我们证明,USP18 的敲低导致 IFN-α2a 信号(通过增加 IFN 刺激反应元件[ISRE]报告基因活性、2',5'-寡聚腺苷酸合成酶[2-5 OAS]表达和 ISG15 诱导来衡量)增加约 100 倍,而 Huh7 HCV 亚基因组复制子测定和 Huh7.5 HCV 感染病毒测定中的抗病毒(AV)效力均增加约 3 倍。虽然不同 RNAi 试剂引起的 USP18 敲低程度与 IFN-α2a 信号的增强相关,但与 AV 活性的增强无关。在使用 Huh7.5 细胞的脑炎心肌炎病毒(EMCV)测定中,也观察到增加的 IFN-α2a 信号未能完全转化为增加的 AV 效力。这些数据表明,在 Huh7.5 细胞中 IFN 介导的 AV 反应仅对 USP18 活性有一定的依赖性。