Journal
CURRENT MEDICINAL CHEMISTRY
Volume 17, Issue 26, Pages 2837-2853Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986710792065045
Keywords
HIV-1; reverse transcriptase; ribonuclease H; RNase H; RNase H inhibitor; natural compounds; diketo acids; hydrazones
Funding
- Fondazione Banco di Sardegna [1106/2009.0094]
- [2008CE75SA]
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The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by the viral-coded reverse transcriptase (RT), which has two associated functions: the RNA-and DNA-dependent DNA polymerase (RDDP and DDDP) function and the ribonuclease H (RNase H) function. The RNase H function catalyzes the selective hydrolysis of the RNA strand of the RNA: DNA heteroduplex replication intermediate. The RT associated activities are both essential for HIV-1 replication and validated targets for drug development, but only the polymerase function has been widely investigated as drug target. In fact, either nucleoside or non-nucleoside RT inhibitors currently used in therapy act on the polymerase associated activity. In this review, we describe the compounds, reported up to today, which inhibit the HIV-1 RNase H function, their chemical structures, the structure-activity relationships and the mechanism of action.
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