Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges

doi:10.2174/0929867324666170113110839

摘要

抗逆转录病毒药物的组合被成功地用于治疗HIV感染者.然而，耐药性是一个主要的问题，使新的抗逆转录病毒药物的发现成为一个持续的优先。伊蒂。HIV-1逆转录酶的核糖核酸酶H(Rnase H)活性催化RNA链的选择性水解：dna异源复制中间体，代表有吸引力的未开发药物开发目标。本审查报告了2013年至2016年艾滋病毒-1 RNase H抑制剂的特性表征方面的最新进展，介绍了它们的化学结构，结构-活性关系和绑定模式。重点介绍了RNase抑制剂的发现和发展的新的药物化学原理和见解。

关键词: 艾滋病，HIV-1，核糖核酸酶H抑制剂，双重抑制剂，药物设计，SAR，抗病毒，金属酶。

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Current Medicinal Chemistry

Title:Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges

Volume: 25 Issue: 14

关键词: 艾滋病，HIV-1，核糖核酸酶H抑制剂，双重抑制剂，药物设计，SAR，抗病毒，金属酶。

摘要: Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority. The ribonuclease H (RNase H) activity of the HIV-1 reverse transcriptase catalyzes the selective hydrolysis of the RNA strand of RNA:DNA heteroduplex replication intermediates, and represents an attractive unexploited target for drug development. This review reports on recent progress in the characterization of HIV-1 RNase H inhibitors from 2013 to 2016, describing their chemical structures, structureactivity relationship and binding modes. Focus is given to emerging medicinal chemistry principles and insights into the discovery and development of RNase H inhibitors.

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Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges, Current Medicinal Chemistry 2018; 25 (14) . https://dx.doi.org/10.2174/0929867324666170113110839

DOI https://dx.doi.org/10.2174/0929867324666170113110839	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X