McGill University AIDS Centre, Lady Davis Institute-Jewish General Hospital, Montreal, Quebec, Canada.
Retrovirology. 2009 Nov 11;6:103. doi: 10.1186/1742-4690-6-103.
Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes.
This study compares the enzymatic activities of HIV-1 integrase from subtypes B and C as well as susceptibility to various integrase inhibitors in vitro. The catalytic activities of both enzymes were analyzed in regard to each of 3' processing and strand transfer activities both in the presence and absence of the integrase inhibitors raltegravir (RAL), elvitegravir (EVG), and MK-2048.
Our results show that integrase function is similar with enzymes of either subtype and that the various integrase strand transfer inhibitors (INSTIs) that were employed possessed similar inhibitory activity against both enzymes.
This suggests that the use of integrase inhibitors against HIV-1 subtype C will result in comparable outcomes to those obtained against subtype B infections.
整合酶抑制剂目前被纳入高效抗逆转录病毒治疗(HAART)中。由于 HIV 高度变异,整合酶抑制剂的疗效必须针对来自不同亚型的一系列整合酶进行评估。
本研究比较了 HIV-1 整合酶亚型 B 和 C 的酶活性以及对各种整合酶抑制剂的体外敏感性。在存在和不存在整合酶抑制剂raltegravir(RAL)、elvitegravir(EVG)和 MK-2048 的情况下,分析了这两种酶在 3' 加工和链转移活性方面的催化活性。
我们的结果表明,整合酶功能与任何一种亚型的酶相似,所使用的各种整合酶链转移抑制剂(INSTIs)对两种酶均具有相似的抑制活性。
这表明使用整合酶抑制剂治疗 HIV-1 亚型 C 将产生与治疗亚型 B 感染相似的结果。