Department of Immunology and Infectious Diseases, Harvard School of Public Health AIDS Initiative, FXB 402, 651 Huntington Avenue, Boston, MA 02115, USA.
Antimicrob Agents Chemother. 2011 May;55(5):2146-53. doi: 10.1128/AAC.01505-10. Epub 2011 Mar 14.
Single-dose nevirapine (NVP) is quite effective in preventing transmission of the human immunodeficiency virus (HIV) from mother to child; however, many women develop resistance to NVP in this setting. Comparing outcomes of clinical studies reveals an increased amount of resistance in subtype C relative to that in other subtypes. This study investigates how nonnucleoside reverse transcriptase inhibitor (NNRTI) drug resistance mutations of subtype C affect replication capacity. The 103N, 106A, 106M, 181C, 188C, 188L, and 190A drug resistance mutations were placed in a reverse transcriptase (RT) that matches the consensus subtype C sequence as well as the HXB2 RT, as a subtype B reference. The replicative fitness of each mutant was compared with that of the wild type in a head-to-head competition assay. The 106A mutant of subtype C would not grow in the competition assay, making it the weakest virus tested. The effect of the 106M mutation was weaker than those of the 181C and 188C mutations in the consensus C RT, but in subtype B, this difference was not seen. To see if the 106A mutation in a different subtype C background would have a different replicative profile, the same NNRTI resistance mutations were added to the MJ4 RT, a reference subtype C molecular clone. In the context of MJ4 RT, the 106A mutant was not the only mutant that showed poor replicative fitness; the 106M, 188C, and 190A mutants also failed to replicate. These results suggest that NNRTIs may be a cost-effective alternative for salvage therapy if deleterious mutations are present in a subtype C setting.
单剂量奈韦拉平(NVP)在预防母婴传播人类免疫缺陷病毒(HIV)方面非常有效;然而,许多女性在这种情况下对 NVP 产生了耐药性。比较临床研究的结果表明,C 亚型的耐药性比其他亚型增加。本研究探讨了 C 亚型非核苷类逆转录酶抑制剂(NNRTI)耐药突变如何影响复制能力。将 103N、106A、106M、181C、188C、188L 和 190A 耐药突变放置在与 C 亚型共识序列以及 HXB2 RT(B 亚型参考)匹配的逆转录酶(RT)中。在头对头竞争测定中比较每个突变体与野生型的复制适应性。C 亚型的 106A 突变体在竞争测定中无法生长,使其成为测试的最弱势病毒。106M 突变的影响弱于共识 C RT 中的 181C 和 188C 突变,但在 B 亚型中则没有观察到这种差异。为了观察 106A 突变在不同 C 亚型背景下是否具有不同的复制谱,将相同的 NNRTI 耐药突变添加到 MJ4 RT(参考 C 亚型分子克隆)中。在 MJ4 RT 的背景下,106A 突变体并不是唯一显示出较差复制适应性的突变体;106M、188C 和 190A 突变体也无法复制。这些结果表明,如果在 C 亚型环境中存在有害突变,NNRTIs 可能是挽救治疗的一种具有成本效益的替代方法。