Inhibition of thymidine phosphorylase (PD-ECGF) from SD-lymphoma by phosphonomethoxyalkyl thymines
Jazyk angličtina Země Velká Británie, Anglie Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
15857616
DOI
10.1016/j.bcp.2005.03.003
PII: S0006-2952(05)00149-8
Knihovny.cz E-zdroje
- MeSH
- inhibitory enzymů farmakologie MeSH
- krysa rodu Rattus MeSH
- lymfom T-buněčný enzymologie MeSH
- organofosfonáty farmakologie MeSH
- potkani Sprague-Dawley MeSH
- stereoizomerie MeSH
- thymidinfosforylasa antagonisté a inhibitory MeSH
- thymin analogy a deriváty farmakologie MeSH
- thymopoetiny farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1-(3-fluoro-2-(phosphonomethoxy)propyl)thymine MeSH Prohlížeč
- inhibitory enzymů MeSH
- organofosfonáty MeSH
- thymidinfosforylasa MeSH
- thymin MeSH
- thymopoetiny 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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