A potent and highly selective inhibitor of human α-1, 3-fucosyltransferase via click chemistry

LV Lee, ML Mitchell, SJ Huang, VV Fokin…

Index: Lee, Lac V.; Mitchell, Michael L.; Huang, Shih-Jung; Fokin, Valery V.; Sharpless, K. Barry; Wong, Chi-Huey Journal of the American Chemical Society, 2003 , vol. 125, # 32 p. 9588 - 9589

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Citation Number: 453

Abstract

Potent inhibitors of fucosyltransferases, and glycosyltransferases in general, have been elusive due to the inherent barriers surrounding the family of glycosyltransfer reactions. The problems of weak substrate affinity and low catalytic proficiency of fucosyltransferase was offset by recruiting additional binding features, in this case hydrophobic interactions, to produce a high affinity inhibitor, 24, with K i= 62 nM. The molecule was identified from a ...