Olsen J C, Furman P, Fyfe J A, Swanstrom R
J Virol. 1987 Sep;61(9):2800-6. doi: 10.1128/JVI.61.9.2800-2806.1987.
We tested the ability of the thymidine analog 3'-azido-3'-deoxythymidine (BWA509U) to inhibit the replication of the retrovirus avian leukosis virus. Inhibition was measured with two different assays: inhibition of a single round of virus replication and inhibition of virus spread through a cell culture. With both assays, we detected inhibition of virus growth, although inhibition of a single round of virus replication required a 40-fold higher drug concentration than did inhibition of virus spread. We also detected variations in the concentrations of drug needed to inhibit virus replication in different cell types. Higher concentrations of drug were needed to inhibit virus replication in chicken embryo fibroblasts than in the continuous quail cell line QT6. Viral DNA synthesis in infected cells was shown to be inhibited in the presence of the drug. The triphosphate form of the analog acted as a competitive inhibitor of purified viral reverse transcriptase, with a Ki of 0.09 +/- 0.003 microM, and was incorporated as a chain terminator during reverse transcription of the natural viral RNA substrate in vitro.
我们测试了胸苷类似物3'-叠氮基-3'-脱氧胸苷(BWA509U)抑制逆转录病毒禽白血病病毒复制的能力。通过两种不同的试验来测定抑制作用:抑制单轮病毒复制和抑制病毒在细胞培养物中的传播。在这两种试验中,我们都检测到了病毒生长的抑制,尽管抑制单轮病毒复制所需的药物浓度比抑制病毒传播所需的药物浓度高40倍。我们还检测到在不同细胞类型中抑制病毒复制所需药物浓度的差异。与连续鹌鹑细胞系QT6相比,抑制鸡胚成纤维细胞中的病毒复制需要更高浓度的药物。在药物存在的情况下,感染细胞中的病毒DNA合成被证明受到抑制。该类似物的三磷酸形式作为纯化病毒逆转录酶的竞争性抑制剂,其Ki为0.09±0.003微摩尔,并且在体外天然病毒RNA底物的逆转录过程中作为链终止剂被掺入。