Selected article for: "activity integrase and integrase RT inhibition"
Author: Ross D. Overacker; Somdev Banerjee; George F. Neuhaus; Selena Milicevic Sephton; Alexander Herrmann; James A. Strother; Ruth Brack-Werner; Paul R. Blakemore; Sandra Loesgen
Title: Biological Evaluation of Molecules of the azaBINOL Class as Antiviral Agents: Specific Inhibition of HIV-1 RNase H Activity by 7-Isopropoxy-8-(naphth-1-yl)quinoline
  • Document date: 2019_1_23
    • ID: m2zw8eq4_18
    Snippet: The copyright holder for this preprint (which was not peer-reviewed) is the author/funder. . https://doi.org/10.1101/525105 doi: bioRxiv preprint Mg 2+ ions, and therefore are often dual inhibitors, with effects on reverse transcriptase and 215 integrase as both require bivalent metals in their active site. We screened B#24 for inhibitory 216 activity in recombinant protein-based assays to test for HIV-1 RT and/or integrase antiviral 217 inhibiti.....
    Document: The copyright holder for this preprint (which was not peer-reviewed) is the author/funder. . https://doi.org/10.1101/525105 doi: bioRxiv preprint Mg 2+ ions, and therefore are often dual inhibitors, with effects on reverse transcriptase and 215 integrase as both require bivalent metals in their active site. We screened B#24 for inhibitory 216 activity in recombinant protein-based assays to test for HIV-1 RT and/or integrase antiviral 217 inhibition (Table 3) . AzaBINOL B#24 showed no effect against HIV-1 integrase activity in a 218 commercially available kit (ExpressBio, Frederick, MD) at any concentration tested up to 200 219 µM. When tested against an HIV-1 RT polymerase assay we observed only weak inhibitory 220 effects for B#24 at concentrations higher than 100 µM, several orders of magnitude weaker than 221 seen in our cell-based assays. 222

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