β-L-D4A对DNA聚合酶α的作用及机制
Effect and mechanism of beta-L-D4A on DNA polymerase alpha.
作者信息
Li Yan, Lin Ju-Sheng, Zhang Ying-Hui, Wang Xiao-Yan, Chang Ying, He Xing-Xing
机构信息
Institute of Liver Diseases, Tongji Medical College, Huazhong University of Science and Technology, 1095 Jiefang Street, Wuhan 430030, Hubei Province, China.
出版信息
World J Gastroenterol. 2007 Dec 14;13(46):6243-8. doi: 10.3748/wjg.v13.i46.6243.
AIM
To investigate the safety of beta-L-D4A on DNA polymerase alpha.
METHODS
Ion exchange chromatography was used to separate DNA polymerase alpha from crude extract of human Hela cells. Detailed kinetic parameters were determined for beta-L-D4A against DNA polymerase alpha.
RESULTS
DNA polymerase alpha was purified with 4% yield and 31000 units/mg specific activity. The Michaelis constant (Km = 3.22 micromol/L), 50% inhibition concentration (IC50 = 178.49 micromol/L) and inhibition constant (Ki = 126 micromol/L) of beta-L-D4A were determined by kinetic analysis.
CONCLUSION
beta-L-D4A is a more safe nucleoside for hepatitis B virus infection with a lower host toxicity.
目的
研究β-L-D4A对DNA聚合酶α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DNA聚合酶α。测定了β-L-D4A针对DNA聚合酶α的详细动力学参数。
结果
以4%的产率和31000单位/毫克的比活性纯化了DNA聚合酶α。通过动力学分析确定了β-L-D4A的米氏常数（Km = 3.22微摩尔/升）、50%抑制浓度（IC50 = 178.49微摩尔/升）和抑制常数（Ki = 126微摩尔/升）。
结论
β-L-D4A是一种对乙型肝炎病毒感染更安全的核苷，宿主毒性较低。
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