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Research Progress of HIV-1 Nef Inhibitors.
AIDS Reviews ( IF 1.9 ) Pub Date : 2020-10-26 , DOI: 10.24875/aidsrev.20000050
Yanhan Lv 1 , Yuanxi Meng 1 , Jiaqian Zhong 1 , Junhui Wan 2 , Wei Zou 3
Affiliation  

HIV-1 infection poses a major threat to the public health worldwide. The antiretroviral agents that are currently used to treat HIV-1 infection target viral reverse transcriptase, integrase and protease, or block the fusion of viral envelop and cell membrane. Studies have shown that the HIV-1 encoded protein Nef plays an important role in the pathogenesis of viral infection. Nef ensures efficient counterattack against host immune responses as well as long-term evasion of immune surveillance. In addition, Nef, expressing at a high level early in the viral life cycle, is required for maintaining a high viral load in the persistent infection in vivo and for full pathologic potential. Therefore, Nef may be an excellent target to treat HIV-1 infection. In this manuscript, we reviewed five potential Nef inhibitors, namely, DLC27-14, t ightly bound hydroxypyrazole HIV-1 Nef inhibitor B9, 2c-like inhibitors, N-(3-aminoquinoxalin-2-yl)-4-chlorobenzenesulfonamide and compound 1[(7-oxo-7H-benzo[anthracene]-3-yl)amino]anthraquinone, and their working mechanisms. These drugs may be further developed into new regimens for the treatment of HIV-1 infection.

中文翻译:

HIV-1 Nef抑制剂的研究进展。

HIV-1 感染对全世界的公共卫生构成重大威胁。目前用于治疗 HIV-1 感染的抗逆转录病毒药物靶向病毒逆转录酶、整合酶和蛋白酶,或阻断病毒包膜和细胞膜的融合。研究表明,HIV-1编码的蛋白Nef在病毒感染的发病机制中起重要作用。Nef 确保有效反击宿主免疫反应以及长期逃避免疫监视。此外,在病毒生命周期早期高水平表达的 Nef 是维持体内持续感染中的高病毒载量和充分发挥病理潜力所必需的。因此,Nef 可能是治疗 HIV-1 感染的极好靶点。在这份手稿中,我们回顾了五种潜在的 Nef 抑制剂,即 DLC27-14、紧密结合的羟基吡唑 HIV-1 Nef 抑制剂 B9、2c 样抑制剂、N-(3-aminoquinoxalin-2-yl)-4-氯苯磺酰胺和化合物 1[(7-oxo-7H-benzo[anthracene]-3-yl) )氨基]蒽醌及其作用机制。这些药物可能会进一步发展成为治疗 HIV-1 感染的新方案。
更新日期:2020-10-31
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