European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2022-09-12 , DOI: 10.1016/j.ejmech.2022.114760
Lina Zhang 1 , Fenju Wei 1 , Jiwei Zhang 1 , Chuanfeng Liu 1 , Nerea López-Carrobles 2 , Xinyong Liu 1 , Luis Menéndez-Arias 2 , Peng Zhan 1
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During HIV-1 genome replication, the viral reverse transcriptase-associated ribonuclease H (RT-associated RNase H) activity hydrolyzes the RNA strand of RNA/DNA heteroduplex intermediates. As of today, HIV-1 RNase H inhibitors (RHIs) remain at an investigational level, although none of them reached clinical trials. Therefore, RNase H remains as an attractive target for drug design and development. In this paper, we review the current status of medicinal chemistry strategies aimed at the discovery of novel RHIs, while discussing problems encountered in their characterization and further development, thereby providing an update on recent progress in the field.
中文翻译：
目前发现新型 HIV-1 核糖核酸酶 H 抑制剂的药物化学策略
在 HIV-1 基因组复制过程中，病毒逆转录酶相关核糖核酸酶 H（RT 相关 RNase H）活性水解 RNA/DNA 异源双链中间体的 RNA 链。截至今天，HIV-1 RNase H 抑制剂 (RHI) 仍处于研究水平，尽管它们都没有进入临床试验。因此，RNase H 仍然是药物设计和开发的一个有吸引力的目标。在本文中，我们回顾了旨在发现新型 RHI 的药物化学策略的现状，同时讨论了在其表征和进一步发展中遇到的问题，从而提供了该领域最新进展的最新信息。
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