Inhibition of thymidine phosphorylase (PD-ECGF) from SD-lymphoma by phosphonomethoxyalkyl thymines
Language English Country England, Great Britain Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
15857616
DOI
10.1016/j.bcp.2005.03.003
PII: S0006-2952(05)00149-8
Knihovny.cz E-resources
- MeSH
- Enzyme Inhibitors pharmacology MeSH
- Rats MeSH
- Lymphoma, T-Cell enzymology MeSH
- Organophosphonates pharmacology MeSH
- Rats, Sprague-Dawley MeSH
- Stereoisomerism MeSH
- Thymidine Phosphorylase antagonists & inhibitors MeSH
- Thymine analogs & derivatives pharmacology MeSH
- Thymopoietins pharmacology MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1-(3-fluoro-2-(phosphonomethoxy)propyl)thymine MeSH Browser
- Enzyme Inhibitors MeSH
- Organophosphonates MeSH
- Thymidine Phosphorylase MeSH
- Thymine MeSH
- Thymopoietins MeSH
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.
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