IndraLab

Statements

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"Further, to gain insight into its inhibitory potential toward NS2B-NS3 protease, we performed enzyme kinetic studies, which revealed that hydroxychloroquine inhibits protease activity with an inhibition constant (K i) of 92.34 +/- 11.91 muM."
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"Antimalaria agents chloroquine and hydroxychloroquine have been studied for their ability to neutralize lysosomal pH and inhibit protease activity."
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"Hydroxychloroquine can also significantly inhibit the main protease and also decrease the production of cytokines during SARS-CoV-2 infection."
32837137
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"As shown in Figure 3B, by alkalisation of the lysosome, HCQ can partially inhibit the activation of proteases as well as block the cleaving of the invariant chain from MHC II."
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"Hydroxychloroquine [Figure 3(26)], a drug already approved and used in pregnancy, can inhibit the bZiPro construct of NS2B-NS3 protease activity with an inhibition constant (Ki) of 92.34 ± 11.91 μM (Table 3; Kumar et al., 2018)."
31866959
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"Importantly, the NS2B-NS3 protease activity of ZIKV can be blocked by an inhibitor of autophagy, hydroxychloroquine (HCQ) (154)."
33117336
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"Overall, Chloroquine and its derivatives demonstrated a higher binding affinity for NSP3 viral protein when compared to other proteins included in this study, thereby signifying their potential as inhibitors of NSP3 function.The main protease is moderately inhibited by Hydroxychloroquine with the binding affinity (−4.8 kcal/mol) (Tables 5 and 5.1 supplementary)."
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"Hydroxychloroquine inhibits the protease activity of NS2B-NS3, which helps in the hydrolysis and maturation of Zika virus and decreases the infection in placental cells [75]."
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"In addition to interfering with autophagic flux, the accumulation of CQ and HCQ within the endosomes/lysosomes can inhibits the post-translational modification of newly synthesized proteins within the[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Hydroxychloroquine Inhibits Zika Virus NS2B-NS3 Protease."
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"Similarly, some studies have suggested that HCQ blocks virus integration into endosomes by modifying the cellular pH and activating lysosomal proteases, leading to virus degradation.30 31 Given that HCQ’s properties are at the frontier of anti-infectious and immunomodulatory activity, it seems legitimate to put an end to this controversy by prospectively and rigorously evaluating the pre-exposure efficacy of HCQ against COVID-19 infection and its effects on the anti-COVID-19 vaccine response."
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"Thus , CQ and HCQ inhibit the protease that is necessary for cleaving the spikes of the virus , a step essential for the successful fusion of the virus into the cell [ 44 ] ."
| PMC
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"It is supposed that the likely mechanism of antiviral action of chloroquine (41) and hydroxychloroquine (42) is to inhibit the main protease."
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"Thus, CQ and HCQ inhibit the protease that is necessary for cleaving the spikes of the virus, a step essential for the successful fusion of the virus into the cell [ 43 ]."
32801052
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"Hoffman et al. reported that CQ and HCQ did not inhibit the entry of SARS-CoV-2 virus into lung cells in vitro , as CQ and HCQ did not target to pH-independent transmembrane serine protease TMPRSS2, w[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In a mouse model of pregnancy, HCQ has been shown to inhibit ZIKV replication by targeting the NS2B-NS3 serine protease (Cao et al., 2017; Kumar et al., 2018)."
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"We found that the relative potency of lopinavir and hydroxychloroquine to inhibit the SARS-CoV-2 main protease was 9.12% and 4.56%, respectively."
| DOI
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"HCQ has also been found to inhibit NS2N-NS3 protease activity, and molecular docking further supported the binding of HCQ to the NS2B-NS3 protease active site [114]."
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"The serine protease granzyme B (GzmB), markers of CD8 T cell-induced cytotoxicity, was reduced by HCQ in the liver of AIH mice."
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"HCQ can inhibit NS2B-NS3 protease of Zika Virus and significantly decrease Zika virus infection in placental cells."
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"HCQ inhibits viral entry, protein glycosylation, and replication by decreasing NS2B/NS3 protease activity."
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"Hydroxychloroquine Inhibits Zika Virus NS2B-NS3 Protease."
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"Hydroxychloroquine Inhibits Zika Virus NS2B-NS3 Protease."
30613818
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"Because the amines in HCQ act as proton acceptors, sufficiently high concentrations of HCQ can neutralize the acidic lysosome and inhibit protease activity and autophagosomal fusion, effectively inhibiting autophagy."
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"In antigen-presenting cells, HCQ also reduced constitutive activation of the endo-lysosomal protease legumain and toll-like receptor 9, thereby reducing cytokine production, but it had little apparent impact on constitutive antigen processing and peptide presentation."
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"Hydroxychloroquine inhibits lysosomal proteases and reduces proteolysis and has a consequent mild immunosuppressive action with decreased chemotaxis, phagocytosis, and ROS production [185]."
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