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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Recent Advances in the Research of HIV-1 RNase H Inhibitors

Author(s): Fang Yu, Xinyong Liu, Peng Zhan and Erik De Clercq

Volume 8, Issue 12, 2008

Page: [1243 - 1251] Pages: 9

DOI: 10.2174/138955708786141052

Price: $65


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

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