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Stable analogues of coenzyme-substrate complex of spermidine/spermine-N 1-acetyltransferase reaction. Synthesis and interaction with the enzyme |
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| Authors: | T. A. Keinanen T. Hyvonen J. Vepsalainen L. Alhonen A. R. Khomutov J. Janne |
| Affiliation: | 1. School of Pharmacy, Biocenter Kuopio, University of Eastern Finland, Kuopio, Finland 2. Virtanen Institute of Molecular Sciences, University of Eastern Finland, Kuopio, Finland 3. Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilov St., 32, Moscow, 119991, Russia |
| Abstract: | A convenient two-step synthesis of conjugates of HS-CoA and D-pantetheine with aminooxy analogues of Spm and Spd was suggested. The use of acetone linker provided target conjugates with quantitative yields. The activity of CoA-derived “bisubstrate” inhibitors, being active at microM concentrations, was at least 100 times better than that of corresponding derivatives of D-pantetheine. |
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