Identification of inhibitors of UDP-galactopyranose mutaseviacombinatorialin situscreening

Jian Fu, Huixiao Fu, Yufen Xia, Inès N'Go, Jun Cao, Weidong Pan, Stéphane P. Vincent

Résultats de recherche: Contribution à un journal/une revueArticleRevue par des pairs


Anin situscreening assay for UDP-galactopyranose mutase (UGM, an essential enzyme ofM. tuberculosiscell 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 compoundsin vitroand in a whole cell antibacterial assay. This study provides a blueprint for designing enamide structures as new UGM inhibitors and anti-mycobacterial agents.

langue originaleAnglais
Pages (de - à)1818-1826
Nombre de pages9
journalOrganic and Biomolecular Chemistry
Numéro de publication8
Les DOIs
Etat de la publicationPublié - 28 févr. 2021

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