| A mammalian cell-based assay was used to identify the coronavirus 3CL protease/pro inhibitors that does not require the use of live virus which demonstrated the assays utility that were highly concordant with the results from live virus testing and identified a set of key structural features shared among broadly active 3CLpro inhibitors. The data suggested that the assay could be applicable to other protease families, thus, representing a general platform for viral protease inhibitor studies. | Because of the assays breadth and ease of use, it is well suited to form the backbone of a forward-thinking pandemic preparedness strategy. This would not only be capable of addressing the current human coronaviral strains but also provide the biomedical community with a series of high-value chemical leads to perform additional focused chemical optimization. These compounds could be further checked whether they have undergone preclinical testing for human use. ✍ | 33910954 (J Virol)
PMID | 33910954 Date of Publishing: 2021 Apr 28 | Title | Inhibitors of Coronavirus 3CL Proteases Protect Cells from Protease-Mediated Cytotoxicity | Author(s) name | Resnick SJ, Iketani S et al. | Journal | J Virol | Impact factor | 4.16 Citation count: 8 | Date of Entry | 2021 Aug 10 |
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Resnick SJ, Iketani S, Hong SJ, Zask A, Liu H, Kim S, Melore S, Lin FY, Nair MS, Huang Y, Lee S, Tay NES, Rovis T, Yang HW, Xing L, Stockwell BR, Ho DD, Chavez A. Inhibitors of Coronavirus 3CL Proteases Protect Cells from Protease-Mediated Cytotoxicity. J Virol. 2021 Jun 24;95(14):e0237420. PMID:33910954 |
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| Antiviral activity of Naringenin against SARS-CoV-2 | 250 and 62.5 micromolar concentrations of Naringenin were very effective in protecting cells from SARS-CoV-2 infection. ✍ | 33096221 (Pharmacol Res)
PMID | 33096221 Date of Publishing: 2020 Oct 20 | Title | Naringenin is a powerful inhibitor of SARS-CoV-2 infection in vitro | Author(s) name | Clementi N, Scagnolari C et al. | Journal | Pharmacol Res | Impact factor | 5.78 Citation count: 31 |
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Clementi N, Scagnolari C, D'Amore A, Palombi F, Criscuolo E, Frasca F, Pierangeli A, Mancini N, Antonelli G, Clementi M, Carpaneto A, Filippini A. Naringenin is a powerful inhibitor of SARS-CoV-2 infection in vitro. Pharmacol Res. 2021 Jan;163:105255. PMID:33096221 |
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| On comparing cytokine levels in auranofin and DMSO-treated cells at 24 and 48 h, SARS-CoV-2-induced cytokines was found in significantly lower levels in auranofin treated cells. | ✍ | 32442105 (Virology)
PMID | 32442105 Date of Publishing: 2020 Aug | Title | The FDA-approved gold drug auranofin inhibits novel coronavirus (SARS-COV-2) replication and attenuates inflammation in human cells | Author(s) name | Rothan HA, Stone S et al. | Journal | Virology | Impact factor | 2.819 Citation count: 54 |
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Rothan HA, Stone S, Natekar J, Kumari P, Arora K, Kumar M. The FDA-approved gold drug auranofin inhibits novel coronavirus (SARS-COV-2) replication and attenuates inflammation in human cells. Virology. 2020 Aug;547:7-11. PMID:32442105 |
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| Compound 13b inhibits SARS-CoV-2 replication in human Calu-3 lung cells. | The hydrophobic and bulky Boc group is necessary to cross the cellular membrane
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7164518/figure/F1/ ✍ | 32198291 (Science)
PMID | 32198291 Date of Publishing: 2020 Apr 24 | Title | Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors | Author(s) name | Zhang L, Lin D et al. | Journal | Science | Impact factor | 20.57 Citation count: 1159 |
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Zhang L, Lin D, Sun X, Curth U, Drosten C, Sauerhering L, Becker S, Rox K, Hilgenfeld R. Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors. Science. 2020 Apr 24;368(6489):409-412. PMID:32198291 |
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| Compound 13b inhibits SARS-CoV-2 replication in human Calu-3 lung cells. | The hydrophobic and bulky Boc group is necessary to cross the cellular membrane
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7164518/figure/F1/ ✍ | 32198291 (Science)
PMID | 32198291 Date of Publishing: 2020 Apr 24 | Title | Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors | Author(s) name | Zhang L, Lin D et al. | Journal | Science | Impact factor | 20.57 Citation count: 1159 |
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NLM format |
Zhang L, Lin D, Sun X, Curth U, Drosten C, Sauerhering L, Becker S, Rox K, Hilgenfeld R. Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors. Science. 2020 Apr 24;368(6489):409-412. PMID:32198291 |
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