Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.
Identifieur interne : 001198 ( Ncbi/Checkpoint ); précédent : 001197; suivant : 001199Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.
Auteurs : Erika Martina [Allemagne] ; Nikolaus Stiefl ; Björn Degel ; Franziska Schulz ; Alexander Breuning ; Markus Schiller ; Radim Vicik ; Knut Baumann ; John Ziebuhr ; Tanja SchirmeisterSource :
- Bioorganic & medicinal chemistry letters [ 0960-894X ] ; 2005.
Descripteurs français
- KwdFr :
- MESH :
- métabolisme : Cysteine endopeptidases, Protéines virales.
- pharmacologie : Aziridines, Inhibiteurs de protéases, Peptides.
- traitement médicamenteux : Syndrome respiratoire aigu sévère.
- Humains, Sites de fixation, Virus du SRAS.
English descriptors
- KwdEn :
- MESH :
- chemical , metabolism : Cysteine Endopeptidases, Viral Proteins.
- chemical , pharmacology : Aziridines, Peptides, Protease Inhibitors.
- drug effects : SARS Virus.
- drug therapy : Severe Acute Respiratory Syndrome.
- Binding Sites, Humans.
Abstract
The coronavirus main protease, M(pro), is considered a major target for drugs suitable to combat coronavirus infections including the severe acute respiratory syndrome (SARS). In this study, comprehensive HPLC- and FRET-substrate-based screenings of various electrophilic compounds were performed to identify potential M(pro) inhibitors. The data revealed that the coronaviral main protease is inhibited by aziridine- and oxirane-2-carboxylates. Among the trans-configured aziridine-2,3-dicarboxylates the Gly-Gly-containing peptide 2c was found to be the most potent inhibitor.
DOI: 10.1016/j.bmcl.2005.09.012
PubMed: 16216498
Affiliations:
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pubmed:16216498Le document en format XML
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<front><div type="abstract" xml:lang="en">The coronavirus main protease, M(pro), is considered a major target for drugs suitable to combat coronavirus infections including the severe acute respiratory syndrome (SARS). In this study, comprehensive HPLC- and FRET-substrate-based screenings of various electrophilic compounds were performed to identify potential M(pro) inhibitors. The data revealed that the coronaviral main protease is inhibited by aziridine- and oxirane-2-carboxylates. Among the trans-configured aziridine-2,3-dicarboxylates the Gly-Gly-containing peptide 2c was found to be the most potent inhibitor.</div>
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<name sortKey="Schiller, Markus" sort="Schiller, Markus" uniqKey="Schiller M" first="Markus" last="Schiller">Markus Schiller</name>
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