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10.1016/j.ijbiomac.2020.08.166 http://scihub22266oqcxt.onion/10.1016/j.ijbiomac.2020.08.166 32853604!7444494!32853604     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=32853604&cmd=llinks): Failed to open stream: HTTP request failed! 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Screening and evaluation of approved drugs as inhibitors of main protease of SARS-CoV-2 |pdf=|usr=}}{{32853604}} gab.com Text Screening and evaluation of approved drugs as inhibitors of main protease of SARS-CoV-2 JO: Int J Biol Macromol http://www.kidney.de/pget.php?&tw=1&pmid=32853604 #FOAvip The COVID-19 pandemic caused by SARS-CoV-2 has emerged as a global catastrophe. The virus requires main protease for processing the viral polyproteins PP1A and PP1AB translated from the viral RNA. In search of a quick, safe and successful therapeutic agent; we screened various clinically approved drugs for the in-vitro inhibitory effect on 3CL(Pro) which may be able to halt virus replication. The methods used includes protease activity assay, fluorescence quenching, surface plasmon resonance (SPR), Thermofluor(R) Assay, Size exclusion chromatography and in-silico docking studies. We found that Teicoplanin as most effective drug with IC(50) ~ 1.5 muM. Additionally, through fluorescence quenching Stern-Volmer quenching constant (K(SV)) for Teicoplanin was estimated as 2.5 x 10(5) L.mol(-1), which suggests a relatively high affinity between Teicoplanin and 3CL(Pro) protease. The SPR shows good interaction between Teicoplanin and 3CL(Pro) with K(D) ~ 1.6 muM. Our results provide critical insights into the mechanism of action of Teicoplanin as a potential therapeutic against COVID-19. We found that Teicoplanin is about 10-20 fold more potent in inhibiting protease activity than other drugs in use, such as lopinavir, hydroxychloroquine, chloroquine, azithromycin, atazanavir etc. Therefore, Teicoplanin emerged as the best inhibitor among all drug molecules we screened against 3CL(Pro) of SARS-CoV-2. Twit Text FOAVip Screening and evaluation of approved drugs as inhibitors of main protease of SARS-CoV-2 ????Int J Biol Macromol http://www.kidney.de/pget.php?&tw=1&pmid=32853604 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=32853604 #FOAvip English Wikipedia <ref>{{Cite pmid|32853604}}</ref> Screening and evaluation of approved drugs as inhibitors of main protease of SARS-CoV-2 #MMPMID32853604 Tripathi PK; Upadhyay S; Singh M; Raghavendhar S; Bhardwaj M; Sharma P; Patel AK Int J Biol Macromol 2020[Dec]; 164 (ä): 2622-2631 PMID32853604show ga The COVID-19 pandemic caused by SARS-CoV-2 has emerged as a global catastrophe. The virus requires main protease for processing the viral polyproteins PP1A and PP1AB translated from the viral RNA. In search of a quick, safe and successful therapeutic agent; we screened various clinically approved drugs for the in-vitro inhibitory effect on 3CL(Pro) which may be able to halt virus replication. The methods used includes protease activity assay, fluorescence quenching, surface plasmon resonance (SPR), Thermofluor(R) Assay, Size exclusion chromatography and in-silico docking studies. We found that Teicoplanin as most effective drug with IC(50) ~ 1.5 muM. Additionally, through fluorescence quenching Stern-Volmer quenching constant (K(SV)) for Teicoplanin was estimated as 2.5 x 10(5) L.mol(-1), which suggests a relatively high affinity between Teicoplanin and 3CL(Pro) protease. The SPR shows good interaction between Teicoplanin and 3CL(Pro) with K(D) ~ 1.6 muM. Our results provide critical insights into the mechanism of action of Teicoplanin as a potential therapeutic against COVID-19. We found that Teicoplanin is about 10-20 fold more potent in inhibiting protease activity than other drugs in use, such as lopinavir, hydroxychloroquine, chloroquine, azithromycin, atazanavir etc. Therefore, Teicoplanin emerged as the best inhibitor among all drug molecules we screened against 3CL(Pro) of SARS-CoV-2. |Amino Acid Sequence[MESH] |Antiviral Agents/chemistry/*pharmacology[MESH] |Betacoronavirus/*drug effects/*enzymology/physiology[MESH] |COVID-19[MESH] |Coronavirus 3C Proteases[MESH] |Coronavirus Infections/drug therapy/virology[MESH] |Cysteine Endopeptidases[MESH] |Drug Evaluation, Preclinical/methods[MESH] |Drug Repositioning/*methods[MESH] |Humans[MESH] |Molecular Docking Simulation[MESH] |Pandemics[MESH] |Pneumonia, Viral/drug therapy/virology[MESH] |Protease Inhibitors/chemistry/*pharmacology[MESH] |SARS-CoV-2[MESH] |Teicoplanin/chemistry/pharmacology[MESH] |Viral Nonstructural Proteins/*antagonists & inhibitors[MESH]Screening and evaluation of approved drugs as inhibitors of main prote(epmc).pdf DeepDyve Pubget Overpricing