联合新型非核苷类逆转录酶抑制剂（RTIs）与 AZT 对多药耐药 HIV-1 株具有强烈协同作用。
Combining New Non-Nucleoside Reverse Transcriptase Inhibitors (RTIs) with AZT Results in Strong Synergism against Multi-RTI-Resistant HIV-1 Strains.
机构信息
College of Life Sciences, Hebei Agricultural University, Baoding 071001, China.
Key Laboratory of Medical Molecular Virology of MOE/MOH, School of Basic Medical Sciences, Fudan University, 130 Dong An Rd., Xuhui District, Shanghai 200032, China.
出版信息
Molecules. 2018 Jul 2;23(7):1599. doi: 10.3390/molecules23071599.
Reverse transcriptase inhibitors (RTIs), including nucleoside RTIs (NRTIs) and non-nucleoside RTIs (NNRTIs), are critical antiretroviral drugs for the treatment of human immunodeficiency virus (HIV) infection. Emergence of multi-RTI resistance calls for the development of more potent therapeutics or regimens against RTI-resistant strains. Here, we demonstrated that combining azidothymidine (AZT) with a new NNRTIs under development, diarylpyridine (DAPA)-2e, diarylanilin (DAAN)-14h, or DAAN-15h, resulted in strong synergism against infection by divergent HIV-1 strains, including those resistant to NRTIs and NNRTIs, suggesting the potential for developing these novel NNRTIs as salvage therapy for HIV/acquired immune deficiency syndrome (AIDS) patients.
逆转录酶抑制剂（RTIs），包括核苷逆转录酶抑制剂（NRTIs）和非核苷逆转录酶抑制剂（NNRTIs），是治疗人类免疫缺陷病毒（HIV）感染的关键抗逆转录病毒药物。多种 RTIs 耐药的出现要求开发更有效的治疗药物或方案来对抗对 RTIs 耐药的菌株。在这里，我们证明了将叠氮胸苷（AZT）与正在开发的新型 NNRTIs，即二芳基嘧啶（DAPA）-2e、二芳基苯胺（DAAN）-14h 或 DAAN-15h 联合使用，对多种 HIV-1 毒株的感染具有强烈的协同作用，包括对 NRTIs 和 NNRTIs 耐药的毒株，这表明这些新型 NNRTIs 有可能作为 HIV/获得性免疫缺陷综合征（AIDS）患者的挽救治疗药物。
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