| Literature DB >> 17728868 |
Adrian Scaffidi1, Keith A Stubbs, Rebecca J Dennis, Edward J Taylor, Gideon J Davies, David J Vocadlo, Robert V Stick.
Abstract
The synthesis of an analogue of 6-epi-valienamine bearing an acetamido group and its characterisation as an inhibitor of beta-N-acetylglucosaminidases are described. The compound is a good inhibitor of both human O-GlcNAcase and human beta-hexosaminidase, as well as two bacterial beta-N-acetylglucosaminidases. A 3-D structure of the complex of Bacteroides thetaiotaomicron BtGH84 with the inhibitor shows the unsaturated ring is surprisingly distorted away from its favoured solution phase conformation and reveals potential for improved inhibitor potency.Entities:
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Year: 2007 PMID： 17728868 DOI： 10.1039/b709681j
Source DB: PubMed Journal: Org Biomol Chem ISSN： 1477-0520 Impact factor: 3.876