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Literature summary extracted from

  • Renck, D.; Machado, P.; Souto, A.A.; Rosado, L.A.; Erig, T.; Campos, M.M.; Farias, C.B.; Roesler, R.; Timmers, L.F.; de Souza, O.N.; Santos, D.S.; Basso, L.A.
    Design of novel potent inhibitors of human uridine phosphorylase-1: synthesis, inhibition studies, thermodynamics, and in vitro influence on 5-fluorouracil cytotoxicity (2013), J. Med. Chem., 56, 8892-8902.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.3 expressed in Escherichia coli Rosetta (DE3) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.3 4-benzyl-6-hydroxy-2-oxo-1,2-dihydropyridine-3-carbonitrile 2% inhibition at 0.001 mM Homo sapiens
2.4.2.3 4-ethyl-6-hydroxy-2-oxo-1,2-dihydropyridine-3-carbonitrile 25% inhibition at 0.001 mM Homo sapiens
2.4.2.3 4-hydroxy-5-[[(2-hydroxyethyl)amino]methyl]-3,4-dihydropyrimidin-2(1H)-one 2% inhibition at 0.001 mM Homo sapiens
2.4.2.3 5-benzyl-1-(2'-hydroxyethoxymethyl)uracil competitive inhibition with respect to uridine, noncompetitive inhibition with respect to phosphate Homo sapiens
2.4.2.3 5-benzyl-6-hydroxy-4-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile 43% inhibition at 0.001 mM Homo sapiens
2.4.2.3 5-[(diethylamino)methyl]-6-hydroxy-4-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile 25% inhibition at 0.001 mM Homo sapiens
2.4.2.3 5-[(dimethylamino)methyl]-6-hydroxy-4-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile 81% inhibition at 0.001 mM Homo sapiens
2.4.2.3 5-[[(1,3-dihydroxypropan-2-yl)amino]methyl]-6-hydroxy-4-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile 82% inhibition at 0.001 mM Homo sapiens
2.4.2.3 5-[[(2,3-dihydroxypropyl)amino]methyl]-6-hydroxy-4-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile 78% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-1H-pyridin-2-one 38% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-2-oxo-1,2-dihydropyridine-3-carbonitrile 67% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-2-oxo-4-(propan-2-yl)-1,2-dihydropyridine-3-carbonitrile 31% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile 42% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-2-oxo-4-propyl-1,2-dihydropyridine-3-carbonitrile 16% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-3,4-dimethylpyridin-2(1H)-one 9.5% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-3-methylpyridin-2(1H)-one 12% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-4-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile 70% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-4-methyl-2-oxo-5-phenyl-1,2-dihydropyridine-3-carbonitrile 12% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-4-methyl-2-oxo-5-[(piperidin-1-yl)methyl]-1,2-dihydropyridine-3-carbonitrile 49% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-4-methyl-5-[(morpholin-4-yl)methyl]-2-oxo-1,2-dihydropyridine-3-carbonitrile 51% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-4-methylpyridin-2(1H)-one 16% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-4-propyl-1H-pyridin-2-one-3-carbonitrile 16% inhibition at 0.001 mM Homo sapiens
2.4.2.3 6-hydroxy-5-(((2-hydroxyethyl)amino)methyl)-4-methyl-1H-pyridin-2-one-3-carbonitrile 80% inhibition at 0.001 mM Homo sapiens
2.4.2.3 potassium 5-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-olate 60% inhibition at 0.001 mM Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.2.3 0.05
-
 uridine in 100 mMn Tris buffer pH 7.4, at 37°C Homo sapiens
2.4.2.3 2
-
 phosphate in 100 mMn Tris buffer pH 7.4, at 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.3 uridine + phosphate Homo sapiens
-
 uracil + alpha-D-ribose 1-phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.3 Homo sapiens Q16831
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.2.3
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.3 colon cancer cell
-
 Homo sapiens
-
2.4.2.3 SW-620 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.3 uridine + phosphate
-
 Homo sapiens uracil + alpha-D-ribose 1-phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.2.3 UP1
-
 Homo sapiens
2.4.2.3 uridine phosphorylase-1
-
 Homo sapiens