Development of transition state analogue inhibitors for N-acetylglycosyltransferases bearing dpsico- or dtagatofuranose scaffolds |
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Authors: | Marek Baráth Chun-Hung Lin Igor Tvaroška Ján Hirsch |
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Affiliation: | 1.Institute of Chemistry,Slovak Academy of Sciences,Bratislava,Slovakia;2.Institute of Biological Chemistry,Academia Sinica,Taipei,Taiwan;3.Department of Chemistry, Faculty of Natural Sciences,Constantine The Philosopher University,Nitra,Slovakia |
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Abstract: | New potential transition state analogue inhibitors for N-acetylglucosyltransferases (GnTs) were synthesised. These compounds based on psico- and tagatofuranose (structure) scaffold contained a 2-thiophenyl-1-O-diethylphosphate moiety mimicking the proposed model of the transition state of the enzymatic reaction catalysed by N-acetylglucosyltransferases. The synthesised compounds as well as their precursors were fully characterised by NMR, optical rotation and mass techniques. Anomeric configuration of tagatofuranose derivatives was confirmed by X-ray crystallography. Two types of potential human glycosyltransferase (GnTs) inhibitors representing donor UDP-GlcNAc, assigned for biological assays on human GnTs, were prepared. |
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