Efficient Sialyltransferase Inhibitors Based on Transition-State Analogues of the Sialyl Donor |
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| Authors: | Bernd Mü ller,Christoph Schaub,Richard R. Schmidt |
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| Abstract: | A 200- to 1000-fold higher affinity for sialyltransferase is shown by compounds 1 and 2 relative to the natural substrate. These inhibitors, which are derived from the transition state of SN1-type sialyltransfer, contain a flat ring that is attached through a carbon atom with a phosphonate and a cytidine monophosphate group. |
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| Keywords: | Enzyme inhibitors Neuraminic acids Phosphonates Transition states |
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