Oesterle R, Jurkiewicz E, Lüke W, Nickel P, Hunsmann G, Jentsch K D
German Primate Centre, Department of Virology and Immunology, Göttingen.
Antiviral Res. 1993 Oct;22(2-3):107-19. doi: 10.1016/0166-3542(93)90089-2.
The reverse transcriptase (RT) inhibition and the specificity of 15 aminonaphthalenesulfonic acid derivatives were examined with RT of a simian immunodeficiency virus derived from an African green monkey (SIVagmTYO-7). The two compounds with the strongest RT inhibition (NF415) or the highest specificity (NF345), together with suramin, were evaluated against polymerase alpha-primase complex from calf thymus. We have also compared the kinetics of inhibition of the viral and the cellular polymerase by these three compounds. While RT inhibition followed a mixed competitive and non-competitive mechanism, inhibition of the DNA polymerase alpha was competitive for suramin and non-competitive for NF415 and NF345. Certain structural characteristics appeared to be common for specific RT inhibitors.
利用源自非洲绿猴的猿猴免疫缺陷病毒（SIVagmTYO - 7）的逆转录酶（RT），检测了15种氨基萘磺酸衍生物的逆转录酶抑制作用和特异性。将两种具有最强RT抑制作用（NF415）或最高特异性（NF345）的化合物与苏拉明一起，针对来自小牛胸腺的聚合酶α-引发酶复合物进行了评估。我们还比较了这三种化合物对病毒和细胞聚合酶的抑制动力学。虽然RT抑制遵循混合竞争和非竞争机制，但DNA聚合酶α的抑制对苏拉明是竞争性的，对NF415和NF345是非竞争性的。特定的RT抑制剂似乎具有某些共同的结构特征。
