Analysis of PUGNAc and NAG-thiazoline as Transition State Analogues for Human O-GlcNAcase: Mechanistic and Structural Insights into Inhibitor Selectivity and Transition State Poise

O-GlcNAcase catalyzes the cleavage of β-O-linked 2-acetamido-2-deoxy-β-d-glucopyranoside (O-GlcNAc) from serine and threonine residues of post-translationally modified proteins. Two potent inhibitors of this enzyme are O-(2-acetamido-2-deoxy-d-glucopyranosylidene)amino-N-phenylcarbamate (PUGNAc) and...

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Veröffentlicht in:	Journal of the American Chemical Society 2007-01, Vol.129 (3), p.635-644
Hauptverfasser:	Whitworth, Garrett E, Macauley, Matthew S, Stubbs, Keith A, Dennis, Rebecca J, Taylor, Edward J, Davies, Gideon J, Greig, Ian R, Vocadlo, David J
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylglucosamine - analogs & derivatives Acetylglucosamine - metabolism beta-N-Acetylhexosaminidases - antagonists & inhibitors beta-N-Acetylhexosaminidases - metabolism Catalysis Crystallography, X-Ray Enzyme Activation Enzyme Inhibitors - metabolism Glycosylation Humans Models, Molecular Oximes - metabolism Phenylcarbamates - metabolism Substrate Specificity Thermodynamics Thiazoles - metabolism
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