Varghese Vici, Pinsky Benjamin A, Smith Darvin S, Klein Daniel, Shafer Robert W
1 Division of Infectious Diseases, Department of Medicine, Stanford University , Stanford, California.
2 Department of Pathology, Stanford University , Stanford, California.
AIDS Res Hum Retroviruses. 2016 Jul;32(7):702-4. doi: 10.1089/AID.2016.0038. Epub 2016 Apr 19.
The integrase strand transfer inhibitor (INSTI)-resistance mutations Q148H/K/R are arguably the most important INSTI-resistance mutations as they represented the first step to high-level dolutegravir cross-resistance. We describe an individual with transmitted four-class drug resistance whose virus sequence had the previously uncharacterized mutation Q148N. Infectious molecular HIV-1 clones containing Q148N alone and in combination with G140S demonstrated ∼2.4-4.5 reduced elvitegravir susceptibility depending on the virus's genetic context but retained susceptibility to raltegravir and dolutegravir. This level of reduced elvitegravir susceptibility is lower than that observed with Q148H/K/R and in fact the infected individual responded to an initial treatment regimen containing tenofovir/emtricitabine/elvitegravir/cobicistat. Q148N was associated with a higher replication capacity than Q148H, suggesting that this mutation may be more fit in the absence of selective INSTI therapy.
整合酶链转移抑制剂(INSTI)耐药突变Q148H/K/R可以说是最重要的INSTI耐药突变,因为它们代表了对多替拉韦产生高水平交叉耐药的第一步。我们描述了一名具有传播性四类药物耐药性的个体,其病毒序列具有先前未被鉴定的突变Q148N。单独含有Q148N以及与G140S组合的感染性分子HIV-1克隆,根据病毒的基因背景,对埃替格韦的敏感性降低了约2.4至4.5倍,但对拉替拉韦和多替拉韦仍保持敏感性。这种埃替格韦敏感性降低的程度低于Q148H/K/R所观察到的程度,事实上,该感染个体对包含替诺福韦/恩曲他滨/埃替格韦/考比司他的初始治疗方案有反应。与Q148H相比,Q148N具有更高的复制能力,这表明在没有选择性INSTI治疗的情况下,这种突变可能更具适应性。