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10.1177/24725552211000652 http://scihub22266oqcxt.onion/10.1177/24725552211000652 33724070!7967019!33724070     free     free     free Deprecated: Implicit conversion from float 225.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 225.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 225.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 225.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 225.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 259.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 259.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 259.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 259.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 292.79999999999995 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       SLAS+Discov 2021 ; 26 (6): 749-756 Nephropedia Template TP {{tp|p=33724070|t=2021. Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry |pdf=|usr=}}{{33724070}} gab.com Text Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry JO: SLAS Discov http://www.kidney.de/pget.php?&tw=1&pmid=33724070 #FOAvip Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) represents a significant threat to human health. Despite its similarity to related coronaviruses, there are currently no specific treatments for COVID-19 infection, and therefore there is an urgent need to develop therapies for this and future coronavirus outbreaks. Formation of the cap at the 5' end of viral RNA has been shown to help coronaviruses evade host defenses. Nonstructural protein 14 (nsp14) is responsible for N7-methylation of the cap guanosine in coronaviruses. This enzyme is highly conserved among coronaviruses and is a bifunctional protein with both N7-methyltransferase and 3'-5' exonuclease activities that distinguish nsp14 from its human equivalent. Mutational analysis of SARS-CoV nsp14 highlighted its role in viral replication and translation efficiency of the viral genome. In this paper, we describe the characterization and development of a high-throughput assay for nsp14 utilizing RapidFire technology. The assay has been used to screen a library of 1771 Food and Drug Administration (FDA)-approved drugs. From this, we have validated nitazoxanide as a selective inhibitor of the methyltransferase activity of nsp14. Although modestly active, this compound could serve as a starting point for further optimization. Twit Text FOAVip Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry ????SLAS Discov http://www.kidney.de/pget.php?&tw=1&pmid=33724070 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33724070 #FOAvip English Wikipedia <ref>{{Cite pmid|33724070}}</ref> Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry #MMPMID33724070 Pearson LA; Green CJ; Lin D; Petit AP; Gray DW; Cowling VH; Fordyce EAF SLAS Discov 2021[Jul]; 26 (6): 749-756 PMID33724070show ga Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) represents a significant threat to human health. Despite its similarity to related coronaviruses, there are currently no specific treatments for COVID-19 infection, and therefore there is an urgent need to develop therapies for this and future coronavirus outbreaks. Formation of the cap at the 5' end of viral RNA has been shown to help coronaviruses evade host defenses. Nonstructural protein 14 (nsp14) is responsible for N7-methylation of the cap guanosine in coronaviruses. This enzyme is highly conserved among coronaviruses and is a bifunctional protein with both N7-methyltransferase and 3'-5' exonuclease activities that distinguish nsp14 from its human equivalent. Mutational analysis of SARS-CoV nsp14 highlighted its role in viral replication and translation efficiency of the viral genome. In this paper, we describe the characterization and development of a high-throughput assay for nsp14 utilizing RapidFire technology. The assay has been used to screen a library of 1771 Food and Drug Administration (FDA)-approved drugs. From this, we have validated nitazoxanide as a selective inhibitor of the methyltransferase activity of nsp14. Although modestly active, this compound could serve as a starting point for further optimization. |*High-Throughput Screening Assays[MESH] |Antiparasitic Agents/chemistry/pharmacology[MESH] |Antiviral Agents/chemistry/*pharmacology[MESH] |COVID-19/virology[MESH] |Cloning, Molecular[MESH] |Drug Repositioning[MESH] |Enzyme Assays[MESH] |Enzyme Inhibitors/chemistry/pharmacology[MESH] |Escherichia coli/genetics/metabolism[MESH] |Exoribonucleases/*antagonists & inhibitors/genetics/metabolism[MESH] |Gene Expression[MESH] |Genetic Vectors/chemistry/metabolism[MESH] |Humans[MESH] |Kinetics[MESH] |Mass Spectrometry/methods[MESH] |Methylation[MESH] |Nitro Compounds/chemistry/*pharmacology[MESH] |Prescription Drugs/chemistry/pharmacology[MESH] |RNA Caps/*antagonists & inhibitors/genetics/metabolism[MESH] |RNA, Viral/*antagonists & inhibitors/genetics/metabolism[MESH] |Recombinant Fusion Proteins/chemistry/genetics/metabolism[MESH] |SARS-CoV-2/*drug effects/enzymology/genetics[MESH] |Small Molecule Libraries/chemistry/pharmacology[MESH] |Thiazoles/chemistry/*pharmacology[MESH] |Viral Nonstructural Proteins/*antagonists & inhibitors/genetics/metabolism[MESH]Development of a High-Throughput Screening Assay to Identify Inhibitor(epmc).pdf DeepDyve Pubget Overpricing