Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities

Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities

The ribonuclease H (RNase H) active site of HIV-1 reverse transcriptase (RT) is the only viral enzyme not targeted by approved antiretroviral drugs. Using a fluorescence-based in vitro assay, we screened 65,239 compounds at a final concentration of 10 µM to identify inhibitors of RT RNase H activity...

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Bibliographic Details
Main Authors: Alondra Vázquez Rivera, Heather Donald, Mounia Alaoui-El-Azher, John J. Skoko, John S. Lazo, Michael A. Parniak, Paul A. Johnston, Nicolas Sluis-Cremer
Format: Article
Language:English
Published: MDPI AG 2024-07-01
Series:Biomolecules
Subjects:
HIV-1
reverse transcriptase
polymerase
ribonuclease H
inhibitor
benzisothiazolone
Online Access:https://www.mdpi.com/2218-273X/14/7/819

Internet

https://www.mdpi.com/2218-273X/14/7/819

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