| Autor: |
Jian, Fu, Huixiao, Fu, Yufen, Xia, Inès, N'Go, Jun, Cao, Weidong, Pan, Stéphane P, Vincent |
| Rok vydání: |
2021 |
| Předmět: |
|
| Zdroj: |
Organicbiomolecular chemistry. 19(8) |
| ISSN: |
1477-0539 |
| Popis: |
An in situ screening assay for UDP-galactopyranose mutase (UGM, an essential enzyme of M. tuberculosis cell wall biosynthesis) has been developed to discover novel UGM inhibitors. The approach is based on the amide-forming reaction of an amino acid core with various cinnamic acids, followed by a direct fluorescence polarization assay to identify the best UGM binders without isolation and purification of the screened ligands. This assay allows us to perform one-pot high-throughput synthesis and screening of enzyme inhibitors in a 384-well plate format. UGM ligands were successfully identified by this technology and their inhibition levels were established from pure synthetic compounds in vitro and in a whole cell antibacterial assay. This study provides a blueprint for designing enamide structures as new UGM inhibitors and anti-mycobacterial agents. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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