Inhibition of thymidine phosphorylase (PD-ECGF) from SD-lymphoma by phosphonomethoxyalkyl thymines.
Biochem Pharmacol
; 69(10): 1517-21, 2005 May 15.
Article
en En
| MEDLINE
| ID: mdl-15857616
ABSTRACT
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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Banco de datos:
MEDLINE
Asunto principal:
Timidina Fosforilasa
/
Timina
/
Timopoyetinas
/
Linfoma de Células T
/
Inhibidores Enzimáticos
/
Organofosfonatos
Límite:
Animals
Idioma:
En
Año:
2005
Tipo del documento:
Article