Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9001666 | Biochemical Pharmacology | 2005 | 5 Pages |
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 â¥Â (R)-HPMPT > (S)-PMPT > (S)-HPMPT > PMET â¥Â (R)-PMPT. The inhibitory potency (Ki/dThdKm) 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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Authors
Ivan Votruba, Karel Pomeisl, Eva TlouÅ¡t'ová, AntonÃn Holý, Berta Otová,