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首页> 外文期刊>The Lancet >Hepatitis G treatment: interferon free or interferon freer?
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Hepatitis G treatment: interferon free or interferon freer?

机译:庚型肝炎的治疗:无干扰素还是无干扰素?

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To circumvent the disadvantages of interferon, direct-acting antiviral drugs have been developed. The HCV RNA polymerase adds a single ribonucleoprotein triphosphate to the 3' nascent end of the RNA chain.3 There is about 65% homology of the HCV NS5B polymerase across HCV genotypes,4 and the polymerase is thus a potentially pangenotypic antiviral target. Several selective inhibitors of HCV NS5B RNA-dependent RNA polymerase have shown potent in-vitro and in-vivo antiviral activity against HCV.5 Sofosbuvir is a single diastereomer, derived from a 2'-deoxy-2'-fluoro-2/-C-methyluridine prodrug.6 A phosphorami-date moiety improves bioavailability and transport of the nucleotide into hepatocytes to engender high concentrations of uridine nucleoside triphosphate, the active polymerase inhibitor.
机译:为了避免干扰素的缺点,已经开发了直接作用的抗病毒药物。 HCV RNA聚合酶在RNA链的3'新生末端添加了一个核糖核蛋白三磷酸。3HCV NS5B聚合酶在HCV基因型之间有大约65%的同源性4,因此该聚合酶是潜在的全基因型抗病毒靶标。几种选择性的HCV NS5B RNA依赖性RNA聚合酶选择性抑制剂已显示出对HCV的有效体外和体内抗病毒活性。5Sofosbuvir是一种单一的非对映异构体,衍生自2'-deoxy-2'-fluoro-2 / -C -甲基尿苷前药。6氨基磷酸酯部分可提高生物利用度,并改善核苷酸向肝细胞的转运,从而产生高浓度的尿苷核苷三磷酸(活性聚合酶抑制剂)。

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