Fourel I, Hantz O, Cova L, Allaudeen H S, Trepo C
Unité de recherche sur les Hépatites et le rôle des virus hépatotropes dans l'oncogenèse INSERM U 271, Lyon, France.
Antiviral Res. 1987 Nov;8(4):189-99. doi: 10.1016/0166-3542(87)90073-8.
The main properties of the duck hepatitis B virus (DHBV) DNA polymerase have been studied and compared with those of the human hepatitis B virus (HBV) and of the woodchuck hepatitis virus (WHV) DNA polymerases. All 3 enzymes are active under high salt conditions in the presence of high magnesium concentration. DHBV DNA polymerase was found less sensitive to ethanol and to operate at higher optimal pH than the HBV and WHV DNA polymerases. Like the other two viral endogenous DNA polymerases, the DHBV enzyme was strongly inhibited by phosphonoformic acid but not by aphidicolin, sulfhydryl group blockers or phosphonoacetic acid. Inhibition of DHBV DNA polymerase by the triphosphate derivatives of several nucleoside analogs appeared similar to that reported for HBV or WHV endogenous polymerase. FIACTP was the most, and ACVTP the least effective inhibitor; BVdUTP was of intermediary potency; araCTP and araTTP had a greater inhibitory effect on DHBV DNA polymerase than HBV or WHV DNA polymerase. The similarities in the properties of DHBV and HBV DNA polymerase justify the use of the duck hepatitis B polymerase model for screening and evaluation of potentially active drugs against HBV infection.
已对鸭乙型肝炎病毒（DHBV）DNA聚合酶的主要特性进行了研究，并与人类乙型肝炎病毒（HBV）和土拨鼠肝炎病毒（WHV）DNA聚合酶的特性进行了比较。在高镁浓度存在的高盐条件下，这三种酶均具有活性。发现DHBV DNA聚合酶对乙醇的敏感性较低，并且在比HBV和WHV DNA聚合酶更高的最佳pH值下发挥作用。与其他两种病毒内源性DNA聚合酶一样，DHBV酶受到膦甲酸的强烈抑制，但不受阿非科林、巯基阻断剂或膦乙酸的抑制。几种核苷类似物的三磷酸衍生物对DHBV DNA聚合酶的抑制作用似乎与报道的HBV或WHV内源性聚合酶的抑制作用相似。氟碘阿糖胞苷三磷酸（FIACTP）是最有效的抑制剂，而阿昔洛韦三磷酸（ACVTP）是最无效的抑制剂；更昔洛韦三磷酸（BVdUTP）具有中等效力；阿糖胞苷三磷酸（araCTP）和阿糖胸苷三磷酸（araTTP）对DHBV DNA聚合酶的抑制作用比对HBV或WHV DNA聚合酶的抑制作用更大。DHBV和HBV DNA聚合酶特性的相似性证明了使用鸭乙型肝炎聚合酶模型来筛选和评估针对HBV感染的潜在活性药物的合理性。
