内源性逆转录分析揭示了携带M184V突变的1型人类免疫缺陷病毒对（-）2'-脱氧-3'-硫代胞苷三磷酸具有高水平抗性。
Endogenous reverse transcription assays reveal high-level resistance to the triphosphate of (-)2'-dideoxy-3'-thiacytidine by mutated M184V human immunodeficiency virus type 1.
作者信息
Quan Y, Gu Z, Li X, Li Z, Morrow C D, Wainberg M A
机构信息
McGill University AIDS Centre, Lady Davis Institute, Jewish General Hospital, Montreal, Quebec, Canada.
出版信息
J Virol. 1996 Aug;70(8):5642-5. doi: 10.1128/JVI.70.8.5642-5645.1996.
Abstract
Kinetic analysis showed that the Ki values and the Ki/Km ratios for mutated, recombinant M184V human immunodeficiency virus type 1 reverse transcriptase (RT) for (-)2'-dideoxy-3'-thiacytidine triphosphate (3TCTP) were 35-fold higher than the equivalent values for wild-type RT but only about twice as high as the equivalent values for each of the triphosphates of ddC (ddCTP) and ddA (ddATP). Fully endogenous RT assays showed that viruses containing the M184V substitution were highly resistant to 3TCTP, with an increase in the 50% inhibitory concentration of 250-fold in comparison with wild-type recombinant virus.
摘要
动力学分析表明，突变的重组M184V 1型人类免疫缺陷病毒逆转录酶（RT）对（-）2'-脱氧-3'-硫代胞苷三磷酸（3TCTP）的Ki值和Ki/Km比是野生型RT相应值的35倍，但仅约为ddC（ddCTP）和ddA（ddATP）各自三磷酸的相应值的两倍。完全内源性RT测定表明，含有M184V替代的病毒对3TCTP具有高度抗性，与野生型重组病毒相比，50%抑制浓度增加了250倍。
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