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Literature summary for 2.4.2.4 extracted from

  • Javaid, S.; Shaikh, M.; Fatima, N.; Choudhary, M.I.
    Natural compounds as angiogenic enzyme thymidine phosphorylase inhibitors in vitro biochemical inhibition, mechanistic, and in silico modeling studies (2019), PLoS ONE, 14, e0225056 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.2.4

Inhibitors

Inhibitors Comment Organism Structure
(2E)-3-phenylprop-2-enoic acid
-
 Escherichia coli
(6aS)-1,2,9,10-tetramethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline uncompetitive inhibition Escherichia coli
2,3,5-trihydroxy-6',7-dimethoxyflavone
-
 Escherichia coli
2H-1-benzopyran-2-one uncompetitive inhibition Escherichia coli
3,3',4',5-tetrahydroxy-6-methoxyflavone mixed-type inhibition Escherichia coli
4,4'-[(2R,3S)-2,3-dimethylbutane-1,4-diyl]di(benzene-1,2-diol) competitive inhibition Escherichia coli
4-methoxy-7H-furo[3,2-g][1]benzopyran-7-one
-
 Escherichia coli
6-methoxy-2-oxo-2H-1-benzopyran-7-yl 6-O-[(2R,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxolan-2-yl]-beta-D-glucopyranoside uncompetitive inhibition Escherichia coli
7-deazaxanthine non-competitive inhibition Escherichia coli
7-hydroxy-6-methoxy-2H-1-benzopyran-2-one non-competitive inhibition Escherichia coli
8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b']dipyran-2-one uncompetitive inhibition Escherichia coli
flavone uncompetitive inhibition Escherichia coli
additional information natural compounds as angiogenic enzyme thymidine phosphorylase inhibitors, in vitro biochemical inhibition, mechanistic, and in silico modeling and molecular docking studies, enzyme-bound structure modelling, overview. No inhibition by 4',5,7-trihydroxyflavone, 5,7-dihydroxyflavone, 9,10-dimethoxy-5,6,9,12-tetrahydro-2H-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-7-ium, [(1R,9aR)-octahydro-2H-quinolizin-1-yl]methanol, 3,4,5-trihydroxybenzoic acid, and 4-hydroxy-3-methoxybenzoic acid. Cytotoxicity MTT assay on 3T3 cell line Escherichia coli
tipiracil
-
 Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate Escherichia coli
-
 thymidine + phosphate
-
 r

Organism

Organism UniProt Comment Textmining
Escherichia coli P0C037
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 Escherichia coli thymidine + phosphate
-
 r

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information inhibition kinetics, Lineweaver-Burk plots Escherichia coli
0.044
-
 4,4'-[(2R,3S)-2,3-dimethylbutane-1,4-diyl]di(benzene-1,2-diol) pH 7.0, 30°C Escherichia coli
0.0768
-
 3,3',4',5-tetrahydroxy-6-methoxyflavone pH 7.0, 30°C Escherichia coli
0.1131
-
 2,3,5-trihydroxy-6',7-dimethoxyflavone pH 7.0, 30°C Escherichia coli
0.1811
-
 8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b']dipyran-2-one pH 7.0, 30°C Escherichia coli
0.1934
-
 7-hydroxy-6-methoxy-2H-1-benzopyran-2-one pH 7.0, 30°C Escherichia coli
0.1951
-
 flavone pH 7.0, 30°C Escherichia coli
0.2385
-
 (6aS)-1,2,9,10-tetramethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline pH 7.0, 30°C Escherichia coli
0.2952
-
 6-methoxy-2-oxo-2H-1-benzopyran-7-yl 6-O-[(2R,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxolan-2-yl]-beta-D-glucopyranoside pH 7.0, 30°C Escherichia coli
0.3442
-
 4-methoxy-7H-furo[3,2-g][1]benzopyran-7-one pH 7.0, 30°C Escherichia coli
0.3497
-
 (2E)-3-phenylprop-2-enoic acid pH 7.0, 30°C Escherichia coli
0.4203
-
 2H-1-benzopyran-2-one pH 7.0, 30°C Escherichia coli