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Synthesis and Biological Evaluation of a Chitobiose-Based Peptide N-Glycanase Inhibitor Library.

  作者 Witte, Martin D.;Horst, Danielle;Wiertz, Emmanuel J. H. J.;van der Marel, Gijsbert A.;Overkleeft, Herman S.;  
  选自 期刊  Journal of Organic Chemistry;  卷期  2009年74-2;  页码  605-616  
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[摘要]Peptide N-glycanase (PNGase), the enzyme responsible for the deglycosylation of N-linked glycoproteins, has an active site related to that of cysteine proteases. Chitobiose was equipped with electrophilic traps often used in cysteine protease inhibitors, and the resulting compds. were evaluated as PNGase inhibitors. We found that the electrophilic trap of the inhibitor has a great influence on the potency of the compds. with the chloromethyl ketone inhibitor being the first potent C-glycoside-based PNGase inhibitor.

 
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