Identification of Inhibitors for UDP-Galactopyranose Mutase

The flavoenzyme uridine 5‘-diphosphate (UDP)-galactopyranose mutase (UGM) plays a key role in the cell wall biosynthesis of many pathogens, including Mycobacterium tuberculosis. Using a synthetic fluorescent ligand, we screened 16 000 compounds in a fluorescence polarization assay. Effective inhibit...

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Veröffentlicht in:	Journal of the American Chemical Society 2004-09, Vol.126 (34), p.10532-10533
Hauptverfasser:	Soltero-Higgin, Michelle, Carlson, Erin E, Phillips, John H, Kiessling, Laura L
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical, structural and metabolic biochemistry Biological and medical sciences Chromatography, High Pressure Liquid Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Enzymes and enzyme inhibitors Fluorescence Polarization - methods Fundamental and applied biological sciences. Psychology General aspects, investigation methods Inhibitory Concentration 50 Intramolecular Transferases - antagonists & inhibitors Intramolecular Transferases - metabolism Kinetics Mycobacterium tuberculosis - enzymology Substrate Specificity
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Beschreibung
Zusammenfassung:	The flavoenzyme uridine 5‘-diphosphate (UDP)-galactopyranose mutase (UGM) plays a key role in the cell wall biosynthesis of many pathogens, including Mycobacterium tuberculosis. Using a synthetic fluorescent ligand, we screened 16 000 compounds in a fluorescence polarization assay. Effective inhibitors of UGM were identified.
ISSN:	0002-7863 1520-5126
DOI:	10.1021/ja048017v