High-Throughput "FP-Tag" Assay for the Identification of Glycosyltransferase Inhibitors.
J Am Chem Soc
; 141(6): 2201-2204, 2019 02 13.
Article
em En
| MEDLINE
| ID: mdl-30698425
ABSTRACT
Bacterial capsular polysaccharides are important virulence factors. Capsular polysaccharides from several important Gram-negative pathogens share a conserved glycolipid terminus containing 3-deoxy-ß-d- manno-oct-2-ulosonic acid (ß-Kdo). The ß-Kdo glycosyltransferases responsible for synthesis of this conserved glycolipid belong to a new family of glycosyltransferases that shares little homology with other such enzymes, thereby representing an attractive antivirulence target. Here, we report the development of a fluorescence polarization-based, high-throughput screening assay (FP-tag) for ß-Kdo glycosyltransferases, and use it to identify a class of marine natural products as lead inhibitors. This "FP-tag" assay should be readily adaptable to high-throughput screens of other glycosyltransferases.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Glicosiltransferases
/
Inibidores Enzimáticos
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article