Novel 3-amino-2-hydroxy acids containing protease inhibitors. Part 1: Synthesis and kinetic characterization as aminopeptidase P inhibitors |
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Authors: | Stöckel-Maschek Angela Stiebitz Beate Koelsch Regine Neubert Klaus |
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Institution: | Martin-Luther-University Halle-Wittenberg, Department of Biochemistry, Institute of Biochemistry/Biotechnology, Kurt-Mothes-Str.3, 06120 Halle/Saale, Germany. stoeckel@biochemtech.uni-halle.de |
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Abstract: | Novel, potent inhibitors of aminopeptidase P, containing a 3-amino-2-hydroxy acid and a proline or a proline analogues, have been prepared. One part of the bestatin-derived inhibitors was found to inhibit APP from Escherichia coli and from rat intestine according to a mixed-type mechanism, with Ki values up to 1.26 microM. The other compounds, 3-amino-2-hydroxy acyl prolines of a different configuration, inhibit APP competitively, according to a slow-binding mechanism, with Ki values in the nanomolar up to the micromolar range. |
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