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10.1042/BCJ20210197 http://scihub22266oqcxt.onion/10.1042/BCJ20210197 34198327!8286836!34198327     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=34198327&cmd=llinks): Failed to open stream: HTTP request failed! 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Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp5 main protease |pdf=|usr=}}{{34198327}} gab.com Text Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp5 main protease JO: Biochem J http://www.kidney.de/pget.php?&tw=1&pmid=34198327 #FOAvip The coronavirus 2019 (COVID-19) pandemic, caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), spread around the world with unprecedented health and socio-economic effects for the global population. While different vaccines are now being made available, very few antiviral drugs have been approved. The main viral protease (nsp5) of SARS-CoV-2 provides an excellent target for antivirals, due to its essential and conserved function in the viral replication cycle. We have expressed, purified and developed assays for nsp5 protease activity. We screened the nsp5 protease against a custom chemical library of over 5000 characterised pharmaceuticals. We identified calpain inhibitor I and three different peptidyl fluoromethylketones (FMK) as inhibitors of nsp5 activity in vitro, with IC50 values in the low micromolar range. By altering the sequence of our peptidomimetic FMK inhibitors to better mimic the substrate sequence of nsp5, we generated an inhibitor with a subnanomolar IC50. Calpain inhibitor I inhibited viral infection in monkey-derived Vero E6 cells, with an EC50 in the low micromolar range. The most potent and commercially available peptidyl-FMK compound inhibited viral growth in Vero E6 cells to some extent, while our custom peptidyl FMK inhibitor offered a marked antiviral improvement. Twit Text FOAVip Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp5 main protease ????Biochem J http://www.kidney.de/pget.php?&tw=1&pmid=34198327 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=34198327 #FOAvip English Wikipedia <ref>{{Cite pmid|34198327}}</ref> Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp5 main protease #MMPMID34198327 Milligan JC; Zeisner TU; Papageorgiou G; Joshi D; Soudy C; Ulferts R; Wu M; Lim CT; Tan KW; Weissmann F; Canal B; Fujisawa R; Deegan T; Nagaraj H; Bineva-Todd G; Basier C; Curran JF; Howell M; Beale R; Labib K; O'Reilly N; Diffley JFX Biochem J 2021[Jul]; 478 (13): 2499-2515 PMID34198327show ga The coronavirus 2019 (COVID-19) pandemic, caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), spread around the world with unprecedented health and socio-economic effects for the global population. While different vaccines are now being made available, very few antiviral drugs have been approved. The main viral protease (nsp5) of SARS-CoV-2 provides an excellent target for antivirals, due to its essential and conserved function in the viral replication cycle. We have expressed, purified and developed assays for nsp5 protease activity. We screened the nsp5 protease against a custom chemical library of over 5000 characterised pharmaceuticals. We identified calpain inhibitor I and three different peptidyl fluoromethylketones (FMK) as inhibitors of nsp5 activity in vitro, with IC50 values in the low micromolar range. By altering the sequence of our peptidomimetic FMK inhibitors to better mimic the substrate sequence of nsp5, we generated an inhibitor with a subnanomolar IC50. Calpain inhibitor I inhibited viral infection in monkey-derived Vero E6 cells, with an EC50 in the low micromolar range. The most potent and commercially available peptidyl-FMK compound inhibited viral growth in Vero E6 cells to some extent, while our custom peptidyl FMK inhibitor offered a marked antiviral improvement. |*Drug Evaluation, Preclinical[MESH] |Amino Acid Chloromethyl Ketones/pharmacology[MESH] |Animals[MESH] |Antiviral Agents/*chemistry/*pharmacology[MESH] |Azoles/pharmacology[MESH] |Chlorocebus aethiops[MESH] |Coronavirus 3C Proteases/*antagonists & inhibitors/genetics/isolation & purification/metabolism[MESH] |Enzyme Assays[MESH] |Fluorescence Resonance Energy Transfer[MESH] |High-Throughput Screening Assays[MESH] |Isoindoles[MESH] |Leupeptins/pharmacology[MESH] |Organoselenium Compounds/pharmacology[MESH] |Peptidomimetics[MESH] |RNA-Binding Proteins/metabolism[MESH] |Reproducibility of Results[MESH] |SARS-CoV-2/drug effects/*enzymology[MESH] |Small Molecule Libraries/chemistry/*pharmacology[MESH] |Vero Cells[MESH]Identifying SARS-CoV-2 antiviral compounds by screening for small mole(epmc).pdf DeepDyve Pubget Overpricing