Abstract
Reverse transcription is a crucial step in the life cycle of human immunodeficiency virus type 1 (HIV-1). In this process, multiple functional enzymes including RNA-dependent DNA polymerase, DNA-dependent DNA polymerase and RNase H are indispensable. The RNase H functions to degrade RNA of the RNA – DNA heteroduplex into small fragment. These properties of HIV-1 RNase H make it an attractive target for rational anti-HIV-1 drug design and development. In this review, we summarized the HIV-1 RNase H inhibitors that were recently reported in the literature, including their chemical structure, mechanism and structure-activity relationship. It seems likely that HIV-1 RNase H as a prominent non-traditional target may lead to the development of anti-HIV agents which could be used alone or in the combination with other HIV inhibitors in AIDS chemotherapy.
Keywords: HIV-1, AIDS, RNase H inhibitor, mechanism, SAR
Mini-Reviews in Medicinal Chemistry
Title: Recent Advances in the Research of HIV-1 RNase H Inhibitors
Volume: 8 Issue: 12
Author(s): Fang Yu, Xinyong Liu, Peng Zhan and Erik De Clercq
Affiliation:
Keywords: HIV-1, AIDS, RNase H inhibitor, mechanism, SAR
Abstract: Reverse transcription is a crucial step in the life cycle of human immunodeficiency virus type 1 (HIV-1). In this process, multiple functional enzymes including RNA-dependent DNA polymerase, DNA-dependent DNA polymerase and RNase H are indispensable. The RNase H functions to degrade RNA of the RNA – DNA heteroduplex into small fragment. These properties of HIV-1 RNase H make it an attractive target for rational anti-HIV-1 drug design and development. In this review, we summarized the HIV-1 RNase H inhibitors that were recently reported in the literature, including their chemical structure, mechanism and structure-activity relationship. It seems likely that HIV-1 RNase H as a prominent non-traditional target may lead to the development of anti-HIV agents which could be used alone or in the combination with other HIV inhibitors in AIDS chemotherapy.
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Cite this article as:
Yu Fang, Liu Xinyong, Zhan Peng and De Clercq Erik, Recent Advances in the Research of HIV-1 RNase H Inhibitors, Mini-Reviews in Medicinal Chemistry 2008; 8 (12) . https://dx.doi.org/10.2174/138955708786141052
DOI https://dx.doi.org/10.2174/138955708786141052 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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