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Design of Glycosyltransferase Inhibitors: Serine Analogues as Pyrophosphate Surrogates?
- Source :
- ChemPlusChem; Oct2015, Vol. 80 Issue 10, p1525-1532, 8p
- Publication Year :
- 2015
-
Abstract
- Mimicking the diphosphate moiety of nucleotide diphosphate sugars with serine analogues provided modest glycosyltransferase inhibitors. The synthetic strategy employed a combination of glycosylation, amide bond formation and azide-alkyne 'click' chemistry. Inhibition constants ( K<subscript>i</subscript>) in the high micromolar range were obtained with a selection of five galactosyltransferases. Cocrystals of three inhibitors bound at the active site of a blood group A/B synthesizing glycosyltransferase were analysed. The structures and inhibitory patterns of the analogues demonstrate the flexibility of the enzymes which complicates the rational design of glycosyltransferase inhibitors. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 21926506
- Volume :
- 80
- Issue :
- 10
- Database :
- Complementary Index
- Journal :
- ChemPlusChem
- Publication Type :
- Academic Journal
- Accession number :
- 110221768
- Full Text :
- https://doi.org/10.1002/cplu.201500282