IndraLab

Statements



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"Hydroxychloroquine can also significantly inhibit the main protease and also decrease the production of cytokines during SARS-CoV-2 infection (Kandeel and Al-Nazawi 2020; Liu et al. 2020b)."

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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) ."

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"Hydroxychloroquine Inhibits Zika Virus NS2B-NS3 Protease."

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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)."

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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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"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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"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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"Importantly, the NS2B-NS3 protease activity of ZIKV can be blocked by an inhibitor of autophagy, hydroxychloroquine (HCQ) (154)."

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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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"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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"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 (À4.8 kcal/mol) (Tables 5 and 5.1 supplementary)."

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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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"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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"Hydroxychloroquine can also significantly inhibit the main protease and also decrease the production of cytokines during SARS-CoV-2 infection Liu et al. 2020b)."

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"The reduced acidification might also be the reason for prevention of SARS-CoV-2 invasion via the cathepsin L-dependent endocytic pathway : since cathepsin L has an acidic pH optimum ( around pH 5.5 ) and is unstable at higher pH ( Turk et al ., 1993 ) , CQ and HCQ could lower the activity of these proteases and block proteolytic activation of the S protein and thus block subsequent fusion between the viral envelope and lysosomal or endosomal membranes ."

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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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"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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"Hydroxychloroquine can also significantly inhibit the main protease and also decrease the production of cytokines during SARS-CoV-2 infection."

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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."