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Effect and mechanism of β-L-D4A on DNA polymerase α

机译:β-L-D4A对DNA聚合酶α的作用及其机制

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AIM: To investigate the safety of β-L-D4A on DNA polymerase a. METHODS: Ion exchange chromatography was used to separate DNA polymerase a from crude extract of human Hela cells. Detailed kinetic parameters were determined for β-L-D4A against DNA polymerase α. RESULTS: DNA polymerase a was purified with 4% yield and 31000 units/mg specific activity. The Michaelis constant (Km = 3.22 μmol/L), 50% inhibition concentration (IC50 = 178.49 μmol/L) and inhibition constant (Ki = 126 μmol/L) of β-L-D4A were determined by kinetic analysis. CONCLUSION: β-L-D4A is a more safe nucleoside for hepatitis B virus (HBV) infection with a lower host toxicity.
机译:目的:探讨β-L-D4A对DNA聚合酶a的安全性。方法:采用离子交换色谱法从人Hela细胞粗提物中分离出DNA聚合酶α。确定了针对DNA聚合酶α的β-L-D4A的详细动力学参数。结果:纯化的DNA聚合酶a的收率为4%,比活性为31000单位/ mg。通过动力学分析确定了β-L-D4A的米氏常数(Km = 3.22μmol/ L),50%抑制浓度(IC50 = 178.49μmol/ L)和抑制常数(Ki = 126μmol/ L)。结论:β-L-D4A是一种较安全的核苷,可用于乙型肝炎病毒(HBV)感染,且宿主毒性较低。

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