World journal of gastroenterology · 2007
Effect and mechanism of beta-L-D4A on DNA polymerase alpha.
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Li Yan, Lin Ju-Sheng, Zhang Ying-Hui, Wang Xiao-Yan, Chang Ying, He Xing-Xing
Аннотация
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.
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.