在羟基脲存在的情况下，3'-叠氮基-3'-脱氧胸苷与2'-脱氧-3'-硫代胞苷联合使用时的激活增加。
Increased activation of the combination of 3'-azido-3'-deoxythymidine and 2'-deoxy-3'-thiacytidine in the presence of hydroxyurea.
作者信息
Palmer S, Cox S
机构信息
Virology Department, Swedish Institute for Infectious Disease Control, Karolinska Institute, Stockholm, Sweden.
出版信息
Antimicrob Agents Chemother. 1997 Feb;41(2):460-4. doi: 10.1128/AAC.41.2.460.
Abstract
The intracellular phosphorylation of 3'-azido-3'-deoxythymidine and 2'-deoxy-3'-thiacytidine was increased two- to threefold by the addition of hydroxyurea (HU) to the single drugs or to the two drugs in combination. The ratios of drug triphosphate to competing cellular deoxynucleoside triphosphate were increased two- to threefold for both 3'-azido-3'-deoxythymidine and 2'-deoxy-3'-thiacytidine in the presence of HU. These HU-induced increases in 3'-azido-3'-deoxythymidine and 2'-deoxy-3'-thiacytidine metabolism may further enhance the anti-human immunodeficiency virus activity of these two drugs.
摘要
在单药或两药联合使用时加入羟基脲（HU），3'-叠氮-3'-脱氧胸苷和2'-脱氧-3'-硫代胞苷的细胞内磷酸化增加了2至3倍。在HU存在下，3'-叠氮-3'-脱氧胸苷和2'-脱氧-3'-硫代胞苷的三磷酸药物与竞争性细胞脱氧核苷三磷酸的比率均增加了2至3倍。HU诱导的3'-叠氮-3'-脱氧胸苷和2'-脱氧-3'-硫代胞苷代谢增加可能会进一步增强这两种药物的抗人类免疫缺陷病毒活性。
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