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Literature summary extracted from

  • Pomeisl, K.; Holy, A.; Votruba, I.; Pohl, R.
    Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase (2008), Bioorg. Med. Chem. Lett., 18, 1364-1367.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.4 expressed in V79 Chinese hamster cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 (R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine 93% inhibition at 0.01 mM Escherichia coli
2.4.2.4 (R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine at 0.01 mM, 82% inhibition of V79 cell-expressed thymidine phosphorylase, 56% inhibition of thymidine phosphorylase from placenta Homo sapiens
2.4.2.4 (R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine 98% inhibition at 0.01 mM Escherichia coli
2.4.2.4 (R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine at 0.01 mM, 84% inhibition of V79 cell-expressed thymidine phosphorylase, 84% inhibition of thymidine phosphorylase from placenta Homo sapiens
2.4.2.4 ([(1R)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid 98% inhibition at 0.01 mM Escherichia coli
2.4.2.4 ([(1R)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase Homo sapiens
2.4.2.4 ([(1R)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid complete inhibition at 0.01 mM Escherichia coli
2.4.2.4 ([(1R)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid at 0.01 mM, 91% inhibition of V79 cell-expressed thymidine phosphorylase, 79% inhibition of thymidine phosphorylase from placenta Homo sapiens
2.4.2.4 ([(1S)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid 93% inhibition at 0.01 mM Escherichia coli
2.4.2.4 ([(1S)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase Homo sapiens
2.4.2.4 ([(1S)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid 94% inhibition at 0.01 mM Escherichia coli
2.4.2.4 ([(1S)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid at 0.01 mM, complete of V79 cell-expressed thymidine phosphorylase, 95% inhibition of thymidine phosphorylase from placenta Homo sapiens
2.4.2.4 1-[2-(phosphonomethoxy)ethyl]thymine complete inhibition at 0.01 mM Escherichia coli
2.4.2.4 1-[2-(phosphonomethoxy)ethyl]thymine at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase, 85% inhibition of thymidine phosphorylase from placenta Homo sapiens
2.4.2.4 [[2-(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid complete inhibition at 0.01 mM Escherichia coli
2.4.2.4 [[2-(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase, 82% inhibition of thymidine phosphorylase from placenta Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Escherichia coli
-
-
-
2.4.2.4 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.4 lymphoma cell SD Homo sapiens
-
2.4.2.4 placenta
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.4 thymidine + phosphate
-
 Escherichia coli thymine + 2-deoxy-D-ribose 1-phosphate
-
 r
2.4.2.4 thymidine + phosphate
-
 Homo sapiens thymine + 2-deoxy-D-ribose 1-phosphate
-
 r

Synonyms

EC Number Synonyms Comment Organism
2.4.2.4 PD-ECGF
-
 Escherichia coli
2.4.2.4 PD-ECGF
-
 Homo sapiens
2.4.2.4 platelet-derived endotherial cell growth factor
-
 Escherichia coli
2.4.2.4 platelet-derived endotherial cell growth factor
-
 Homo sapiens