Recent Progress in the Research of Small Molecule HIV-1 RNase H Inhibitors
Recent Progress in the Research of Small Molecule HIV-1 RNase H Inhibitors
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小分子HIV-1 RNase H抑制剂研究新进展
DOI：
10.2174/0929867321666140120121158
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发表时间：
2014-06-01
影响因子：
4.1
通讯作者：
Liu, Xinyong
中科院分区：
文献类型：
--
作者：
Cao, Lili;Song, Weiguo;Liu, Xinyong
人类免疫缺陷病毒 1 型 (HIV-1) 的逆转录是由病毒编码的逆转录酶 (RT) 启动的生命周期中的关键步骤，其功能为 RNA 和 DNA 依赖性 DNA 聚合酶（RDDP 和 DDDP）以及核糖核酸酶 H (RNase H)。 RNase H 的功能是降解 RNA:DNA 异源双链体的 RNA 链，这使其成为合理的抗 HIV-1 药物设计和开发的有吸引力的靶标。尽管针对DNA聚合酶的药物开发已经非常成功，但HIV RNase H的药物抑制剂的发现仍处于起步阶段，目前还没有任何RNase H抑制剂达到临床开发阶段。本文综述了HIV-1 RNase H抑制剂的最新进展，重点介绍了它们的化学特征、作用机制和构效关系（SAR）。
Reverse transcription of human immunodeficiency virus type 1 (HIV-1) is a crucial step in the life cycle initiated by the viral-coded reverse transcriptase (RT), functioning as RNA-and DNA-dependent DNA polymerase (RDDP and DDDP) and the ribonuclease H (RNase H). The RNase H functions to degrade the RNA strand of the RNA: DNA heteroduplex, which makes it an attractive target for rational anti-HIV-1 drug design and development. Although development of drugs targeting the DNA polymerase have been highly successful, the discovery of drugable inhibitors of HIV RNase H is still in its infancy and none of RNase H inhibitors has reached the clinical development stage currently. This review describes the recent progress in the HIV-1 RNase H inhibitors, focusing on their chemical feature, mechanism and the structure-activity relationship (SAR).