Carbohydrate Chemistry: Chemical and Biological Approaches, Volume 40
Chapter 20: Conformationally restricted glycoside derivatives as mechanistic probes and/or inhibitors of sugar processing enzymes and receptors
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Published:20 Mar 2014
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Carine Maaliki, Charles Gauthier, Olivier Massinon, Ram Sagar, Stéphane P. Vincent, Yves Blériot, 2014. "Conformationally restricted glycoside derivatives as mechanistic probes and/or inhibitors of sugar processing enzymes and receptors", Carbohydrate Chemistry: Chemical and Biological Approaches, Volume 40, Amelia Pilar Rauter, Thisbe Lindhorst, Yves Queneau
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The knowledge of enzyme mechanism is not only fundamental to understand the basic principles of biocatalysis, but it can also lead to the design and the synthesis of potent inhibitors of biologically relevant enzymes. The development of the mechanism-based glycosidase inhibitor Relenza and its validation as a drug to treat influenza virus infections is probably one of the most significant achievement of this research field,1 still inspiring new prototypes.2 Together with the crystal structure analysis of glycosyl-processing enzymes/inhibitor/substrate complexes and the measurements of kinetic isotopic effects (KIE) of isotopically labelled sugars and analogues, the biological evaluation and spectroscopic...