Boyer P L, Gao H Q, Hughes S H
ABL-Basic Research Program, NCI-Frederick Cancer Research and Development Center, Maryland 21702-1201, USA.
Antimicrob Agents Chemother. 1998 Feb;42(2):447-52. doi: 10.1128/AAC.42.2.447.
We have analyzed amino acid substitutions at position G190 in the reverse transcriptase (RT) of human immunodeficiency virus type 1 (HIV-1). The mutation G190E, which is responsible for resistance to certain nonnucleoside inhibitors, results in RT that has significantly less polymerase activity and that is less processive than wild-type RT. Its kinetic profile with respect to dGTP and poly(rC).oligo(dG) is significantly altered compared to that of wild-type RT. The combination of either of the mutations L74V or V75I with the G190E mutation appears to be compensatory and mitigates many of the deleterious effects of the G190E mutation.
我们分析了1型人类免疫缺陷病毒(HIV-1)逆转录酶(RT)中G190位点的氨基酸替代情况。导致对某些非核苷抑制剂耐药的G190E突变,会使RT的聚合酶活性显著降低,且持续性低于野生型RT。与野生型RT相比,其关于dGTP和聚(rC)·寡聚(dG)的动力学特征发生了显著改变。L74V或V75I这两种突变中的任何一种与G190E突变的组合似乎具有补偿作用,并减轻了G190E突变的许多有害影响。