Article ; Online: Identification and evaluation of potential SARS-CoV-2 antiviral agents targeting mRNA cap guanine N7-Methyltransferase.
2021 Volume 193, Page(s) 105142
Abstract: ... the inhibitory effects of compounds against the cap guanine N7-methyltransferase enzyme, which is involved ... SARS-CoV-2, the cause of the currently ongoing COVID-19 pandemic, encodes its own mRNA capping ... in SARS-CoV-2 mRNA capping. We screened five commercially available libraries (7039 compounds in total ...
| Abstract | SARS-CoV-2, the cause of the currently ongoing COVID-19 pandemic, encodes its own mRNA capping machinery. Insights into this capping system may provide new ideas for therapeutic interventions and drug discovery. In this work, we employ a previously developed Py-FLINT screening approach to study the inhibitory effects of compounds against the cap guanine N7-methyltransferase enzyme, which is involved in SARS-CoV-2 mRNA capping. We screened five commercially available libraries (7039 compounds in total) to identify 83 inhibitors with IC |
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| MeSH term(s) | Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; COVID-19/virology ; Cell Line ; Exoribonucleases/antagonists & inhibitors ; Exoribonucleases/metabolism ; High-Throughput Screening Assays ; Humans ; Inhibitory Concentration 50 ; Methyltransferases/antagonists & inhibitors ; Methyltransferases/metabolism ; Nucleotidyltransferases/antagonists & inhibitors ; Nucleotidyltransferases/metabolism ; RNA Caps ; RNA, Viral/genetics ; RNA, Viral/metabolism ; SARS-CoV-2/drug effects ; SARS-CoV-2/genetics ; SARS-CoV-2/metabolism ; Viral Nonstructural Proteins/antagonists & inhibitors ; Viral Nonstructural Proteins/metabolism ; Virus Replication/drug effects ; COVID-19 Drug Treatment | |||||
| Chemical Substances | Antiviral Agents ; RNA Caps ; RNA, Viral ; Viral Nonstructural Proteins ; Methyltransferases (EC 2.1.1.-) ; mRNA (guanine(N7))-methyltransferase (EC 2.1.1.56) ; Nucleotidyltransferases (EC 2.7.7.-) ; mRNA guanylyltransferase (EC 2.7.7.50) ; Exoribonucleases (EC 3.1.-) ; NSP14 protein, SARS-CoV-2 (EC 3.1.-) | |||||
| Language | English | |||||
| Publishing date | 2021-07-23 | |||||
| Publishing country | Netherlands | |||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | |||||
| ZDB-ID | 306628-9 | |||||
| ISSN | 1872-9096 ; 0166-3542 | |||||
| ISSN (online) | 1872-9096 | |||||
| ISSN | 0166-3542 | |||||
| DOI | 10.1016/j.antiviral.2021.105142 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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