Rationally Designed Inhibitors of Inosine Monophosphate Dehydrogenase
| Autor: | Han-Zhong Zhang, Eva Papp, John C. Wu, Kotesvar Rao, Kenneth Straub, Stephen F. Carr, Josef Fried |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
chemistry.chemical_classification
Ribonucleotide biology Substrate (chemistry) NAD Chemical synthesis Mass Spectrometry Inosinic acid chemistry.chemical_compound IMP Dehydrogenase Enzyme Biochemistry chemistry Covalent bond IMP dehydrogenase Enzyme inhibitor Drug Design Drug Discovery biology.protein Humans Molecular Medicine Enzyme Inhibitors Chromatography High Pressure Liquid |
| Zdroj: | Journal of Medicinal Chemistry. 40:4-8 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm960732v |
| Popis: | Functionalized 2-alkyl derivatives of inosinic acid have been synthesized to serve as reversible as well as irreversible inhibitors of the human type II enzyme inosine monophosphate dehydrogenase. These compounds were designed to react with Cys-331 of the enzyme to form covalent bonds so as to interfere with the normal enzyme mechanism which involves attack of Cys-331 at C-2 of the substrate. Mass spectrometric analysis of the reaction products after enzymatic degradation confirmed the appropriateness of the inhibitor design. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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