Selected article for: "crystal structure and protease activity"
Author: Sandra De Meyer; Denisa Bojkova; Jindrich Cinati; Ellen Van Damme; Christophe Buyck; Marnix Van Loock; Brian Woodfall; Sandra Ciesek
Title: Lack of Antiviral Activity of Darunavir against SARS-CoV-2
  • Document date: 2020_4_8
    • ID: 679qfp2s_30
    Snippet: Current data on the therapeutic effect of HIV protease inhibitors in patients with COVID-19 are far from comprehensive. This study demonstrated that DRV showed no in vitro antiviral activity against SARS-CoV-2 at clinically relevant concentrations. Furthermore, structural analyses using protease structures are consistent with these data. DRV binds to the active site of the HIV virus' dimeric aspartic protease (14) . The crystal structure of this .....
    Document: Current data on the therapeutic effect of HIV protease inhibitors in patients with COVID-19 are far from comprehensive. This study demonstrated that DRV showed no in vitro antiviral activity against SARS-CoV-2 at clinically relevant concentrations. Furthermore, structural analyses using protease structures are consistent with these data. DRV binds to the active site of the HIV virus' dimeric aspartic protease (14) . The crystal structure of this protease is well-elucidated and has been shown to have an extensive hydrogen-bonding network with DRV, allowing for the potent in vitro activity (EC 50 values = 1.2 to 8.5 nM) of this protease inhibitor against HIV (6-7).

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