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Literature summary for 2.4.2.4 extracted from

  • Liekens, S.; Hernandez, A.I.; Ribatti, D.; De Clercq, E.; Camarasa, M.J.; Perez-Perez, M.J.; Balzarini, J.
    The nucleoside derivative 5'-O-trityl-inosine (KIN59)suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action (2004), J. Biol. Chem., 279, 29598-29605.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
5'-O-trityl-inosine i.e. KIN59, IC50: 0.044 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action Escherichia coli
5'-O-trityl-inosine i.e. KIN59, IC50: 0.067 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action Homo sapiens
KIN56 IC50: 0.232 mM Escherichia coli
KIN56 IC50: 0.351 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
deoxythymidine + phosphate
-
Escherichia coli thymine + 2-deoxy-D-ribose 1-phosphate
-
?
deoxythymidine + phosphate
-
Homo sapiens thymine + 2-deoxy-D-ribose 1-phosphate
-
?
thymidine + phosphate
-
Escherichia coli thymine + 2-deoxy-D-ribose 1-phosphate
-
?
thymidine + phosphate
-
Homo sapiens thymine + 2-deoxy-D-ribose 1-phosphate
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.044
-
i.e. KIN59, IC50: 0.044 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action Escherichia coli 5'-O-trityl-inosine
0.067
-
i.e. KIN59, IC50: 0.067 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action Homo sapiens 5'-O-trityl-inosine
0.232
-
IC50: 0.232 mM Escherichia coli KIN56
0.351
-
IC50: 0.351 mM Homo sapiens KIN56