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Literature summary extracted from

  • Reigan, P.; Gbaj, A.; Stratford, I.J.; Bryce, R.A.; Freeman, S.
    Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors (2008), Eur. J. Med. Chem., 43, 1248-1260.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 2-mercapto-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one 25% inhibition at 0.045 mM Escherichia coli
2.4.2.4 2-mercapto-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one
-
Homo sapiens
2.4.2.4 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
-
Escherichia coli
2.4.2.4 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
-
Homo sapiens
2.4.2.4 6-amino-5-bromouracil
-
Escherichia coli
2.4.2.4 6-amino-5-bromouracil
-
Homo sapiens
2.4.2.4 7-deazaxanthine
-
Escherichia coli
2.4.2.4 7-deazaxanthine
-
Homo sapiens
2.4.2.4 additional information not inhibited by 5-chloro-6-methyl-3H-pyrimidin-4-one, 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]-3H-pyrimidin-4-one, 6H-imidazo[1,2-c]pyrimidin-5-one, 7H-pyrrolo[2,3-d]pyrimidin-2(1H)-one, and 7H-pyrrolo[2,3-d]pyrimidine Escherichia coli
2.4.2.4 xanthine 13% inhibition at 0.158 mM Escherichia coli
2.4.2.4 xanthine
-
Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.17.3.2 0.0238
-
6-amino-5-bromo-3H-pyrimidin-4-one
-
Bos taurus
1.17.3.2 0.0298
-
1H-pyrrolo[2,3-d]pyrimidin-2-ol substrate and inhibitor compound Bos taurus
1.17.3.2 0.0325
-
6-amino-5-bromo-1H-pyrimidin-2-one
-
Bos taurus
1.17.3.2 0.0444
-
6-amino-5-bromopyrimidine
-
Bos taurus
1.17.3.2 0.0451
-
3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one substrate and inhibitor compound Bos taurus
1.17.3.2 0.0649
-
5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-3H-pyrimidin-4-one substrate and inhibitor compound Bos taurus
1.17.3.2 0.0672
-
7H-pyrrolo[2,3-d]pyrimidine substrate and inhibitor compound Bos taurus
2.4.2.4 0.16
-
5-nitro-2'-deoxyuridine in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens
2.4.2.4 0.23
-
5-nitro-2'-deoxyuridine in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.17.3.2 xanthine + H2O + O2 Bos taurus
-
urate + H2O2
-
?

Organism

EC Number Organism UniProt Comment Textmining
1.17.3.2 Bos taurus
-
-
-
2.4.2.4 Escherichia coli
-
-
-
2.4.2.4 Homo sapiens P19971
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.17.3.2 milk buttermilk Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.17.3.2 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-3H-pyrimidin-4-one + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 6-amino-5-bromo-1H-pyrimidin-2-one + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 6-amino-5-bromo-3H-pyrimidin-4-one + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 6-amino-5-bromopyrimidine + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 7H-pyrrolo[2,3-d]pyrimidin-2(1H)-one + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 7H-pyrrolo[2,3-d]pyrimidine + H2O + O2
-
Bos taurus ?
-
?
1.17.3.2 additional information 5-chloro-6-methyl-3H-pyrimidin-4-one is no substrate Bos taurus ?
-
?
1.17.3.2 xanthine + H2O + O2
-
Bos taurus urate + H2O2
-
?
2.4.2.4 5-nitro-2'-deoxyuridine + phosphate
-
Escherichia coli 5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
-
?
2.4.2.4 5-nitro-2'-deoxyuridine + phosphate
-
Homo sapiens 5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
-
?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.4.2.4 20
-
5-nitro-2'-deoxyuridine in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.00002
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
2.4.2.4 0.000023
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
2.4.2.4 0.0016
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli 6-amino-5-bromouracil
2.4.2.4 0.0065
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli 7-deazaxanthine
2.4.2.4 0.0068
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens 6-amino-5-bromouracil
2.4.2.4 0.045
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens 7-deazaxanthine