|
|||||
|
|
Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor |
|
| Authors: | Martina Erika Stiefl Nikolaus Degel Björn Schulz Franziska Breuning Alexander Schiller Markus Vicik Radim Baumann Knut Ziebuhr John Schirmeister Tanja |
| Institution: | aInstitute of Pharmacy and Food Chemistry, Am Hubland, D-97074 Würzburg, University of Würzburg, Germany bInstitute of Virology and Immunology, Versbacher Street 7, D-97078 Würzburg, University of Würzburg, Germany |
| Abstract: | 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. |
| Keywords: | SARS Main protease Inhibitor Aziridine |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |