Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.
Data(s) |
15/12/2005
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Resumo |
The coronavirus main protease, Mpro, 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 Mpro 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. |
Identificador |
http://dx.doi.org/10.1016/j.bmcl.2005.09.012 http://www.scopus.com/inward/record.url?scp=27444439747&partnerID=8YFLogxK |
Idioma(s) |
eng |
Direitos |
info:eu-repo/semantics/restrictedAccess |
Fonte |
Ziebuhr , J 2005 , ' Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor. ' Bioorganic & Medicinal Chemistry Letters , vol 15 , no. 24 , pp. 5365-5369 . DOI: 10.1016/j.bmcl.2005.09.012 |
Palavras-Chave | #/dk/atira/pure/subjectarea/asjc/1300/1303 #Biochemistry #/dk/atira/pure/subjectarea/asjc/1300/1312 #Molecular Biology #/dk/atira/pure/subjectarea/asjc/1600/1605 #Organic Chemistry #/dk/atira/pure/subjectarea/asjc/3000/3002 #Drug Discovery #/dk/atira/pure/subjectarea/asjc/3000/3003 #Pharmaceutical Science |
Tipo |
article |