Inhibition of thymidine phosphorylase (PD-ECGF) from SD-lymphoma by phosphonomethoxyalkyl thymines
| Autor: | Otová B, Antonín Holý, Karel Pomeisl, Eva Tloušt’ová, Ivan Votruba |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Organophosphonates
Thymopoietins Lymphoma T-Cell Biochemistry Rats Sprague-Dawley Structure-Activity Relationship chemistry.chemical_compound Glycosyltransferase Animals Structure–activity relationship Nucleotide Enzyme Inhibitors Thymidine phosphorylase Phosphorolysis Pharmacology chemistry.chemical_classification Thymidine Phosphorylase biology Stereoisomerism Molecular biology Rats Thymine Enzyme chemistry biology.protein Thymidine |
| Zdroj: | Biochemical Pharmacology. 69:1517-1521 |
| ISSN: | 0006-2952 |
| Popis: | A series of thymine phosphonomethoxyalkyl derivatives were evaluated for their ability to inhibit thymidine phosphorylase (dThdPase) purified from rat spontaneous T-cell lymphoma. A kinetic study of thymidine phosphorolysis catalyzed by dThdPase was performed with thymidine and/or inorganic phosphate as substrates. Data show that the substantial inhibitory effect of these acyclic nucleotide analogues is decreasing in the order of (R)-FPMPT>(S)-FPMPT>or=(R)-HPMPT>(S)-PMPT>(S)-HPMPT>PMET>or=(R)-PMPT. The inhibitory potency (K(i)/(dThd)K(m)) of the most efficient inhibitors from this series against T-cell lymphoma enzyme is 0.0026 for (R)-FPMPT and 0.0048 for (S)-FPMPT. The studied compounds do not inhibit Escherichia coli and human enzyme and possess lower inhibitory potency against rat liver thymidine phosphorylase. |
| Databáze: | OpenAIRE |
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