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Title: | Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: current status and future challenges |
Authors: | Murugesan, Sankaranarayanan |
Keywords: | Pharmacy Dual inhibition Reverse transcriptase (RT) Integrase Molecular hybridization Resistancereverse transcriptase |
Issue Date: | Jan-2021 |
Publisher: | Future Science Group |
Abstract: | Reverse transcriptase and integrase are key enzymes that play a pivotal role in HIV-1 viral maturation and replication. Reverse transcriptase consists of two active sites: RNA-dependent DNA polymerase and RNase H. The catalytic domains of integrase and RNase H share striking similarity, comprising two aspartates and one glutamate residue, also known as the catalytic DDE triad, and a Mg2+ pair. The simultaneous inhibition of reverse transcriptase and integrase can be a rational drug discovery approach for combating the emerging drug resistance problem. In the present review, the dual inhibition of RNase H and integrase is systematically discussed, including rationality of design, journey of development, advancement and future perspective |
URI: | https://www.future-science.com/doi/10.4155/fmc-2020-0257 http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/13346 |
Appears in Collections: | Department of Pharmacy |
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