(-)-2'-DEOXY-3'-THIACYTIDINE IS A POTENT, HIGHLY SELECTIVE INHIBITOR OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 AND TYPE-2 REPLICATION INVITRO
(-)-2'-DEOXY-3'-THIACYTIDINE IS A POTENT, HIGHLY SELECTIVE INHIBITOR OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 AND TYPE-2 REPLICATION INVITRO
复制标题
DOI：
10.1128/aac.36.4.733
复制
发表时间：
1992-04-01
影响因子：
4.9
通讯作者：
CAMERON, JM
中科院分区：
文献类型：
--
作者：
COATES, JAV;CAMMACK, N;CAMERON, JM
2'-脱氧-3'-硫胞苷 (3TC) 的 (-)-对映体在体外被发现是人类免疫缺陷病毒 1 型 (HIV-1) 和 2 (HIV-2) 的有效选择性抑制剂。 我们在一系列携带 CD4 的淋巴细胞系中测定了其对多种 HIV-1 和 HIV-2 实验室毒株的抗病毒活性（平均 50% 抑制浓度 [IC50] 范围，4 nM 至 0.67-mu-M）。 3TC 还对外周血淋巴细胞中的一系列 HIV-1 病毒株具有活性（平均 IC50 范围为 2.5 至 90 nM）。 七种淋巴细胞培养物（包括人外周血淋巴细胞）的细胞毒性 IC50 范围为 0.5 至 6 mM。 3TC 对一系列其他病毒或长期感染 HIV-1 或 HIV-2 的细胞没有可检测到的抗病毒活性。 确定了添加化合物的时间和改变感染的复数对3TC抗病毒活性的影响。 结果表明，3TC 是一种有效的、选择性的 HIV-1 和 HIV-2 体外复制抑制剂。
The (-)-enantiomer of 2'-deoxy-3'-thiacytidine (3TC) was found to be a potent and selective inhibitor of human immunodeficiency virus types 1 (HIV-1) and 2 (HIV-2) in vitro. We determined its antiviral activity against a number of laboratory strains of HIV-1 and HIV-2 in a range of CD4-bearing lymphocyte cell lines (mean 50% inhibitory concentration [IC50] range, 4 nM to 0.67-mu-M). 3TC was also active against a range of HIV-1 strains in peripheral blood lymphocytes (mean IC50 range, 2.5 to 90 nM). The IC50 for cytotoxicity in seven lymphocyte cell cultures, including human peripheral blood lymphocytes, ranged from 0.5 to 6 mM. 3TC had no detectable antiviral activity against a range of other viruses or in cells chronically infected with HIV-1 or HIV-2. The effects of time of addition of the compound and varying the multiplicity of infection on the antiviral activity of 3TC were determined. The results showed that 3TC is a potent and selective inhibitor of HIV-1 and HIV-2 replication in vitro.