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Literature summary extracted from
- Recent discovery of non-nucleobase thymidine phosphorylase inhibitors targeting cancer (2016), Eur. J. Med. Chem., 124, 992-1003 .
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 2.4.2.4 | medicine | thymidine phosphorylase is identified as a prime target for developing anticancer therapies | Homo sapiens |
Crystallization (Commentary)
| EC Number | Crystallization (Comment) | Organism |
|---|---|---|
| 2.4.2.4 | analysis of crystal structure of recombinant Escherichia coli TP in complex with 2'-fluoro-3'-azido-2',3'-dideoxyuridine (N3FddU) and 3'-azidothymidine (AZT) at 1.50 A and 1.52 A resolutions, respectively. Analysis of the free enzyme crystal structure at 2.8 A resolution | Escherichia coli |
| 2.4.2.4 | analysis of crystal structure of recombinant human TP in complex with 5-iodouracil (5IUR) at 3.0 A and 2.5 A resolutions, respectively | Homo sapiens |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 2.4.2.4 | additional information | transfection of TP into KB cells renders them highly resistant to apoptosis caused by hypoxia | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.4.2.4 | (2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one | KIN59 | Escherichia coli |  |
| 2.4.2.4 | (2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one | KIN59 | Homo sapiens | |
| 2.4.2.4 | (3-benzyl-2,4,5-trioxoimidazolidin-1-yl)acetic acid | - |
Homo sapiens | |
| 2.4.2.4 | 1-(2-phenylethyl)imidazolidine-2,4,5-trione | - |
Homo sapiens | |
| 2.4.2.4 | 1-benzylimidazolidine-2,4,5-trione | - |
Homo sapiens | |
| 2.4.2.4 | 1-[(2-methylphenyl)methyl]imidazolidine-2,4,5-trione | - |
Homo sapiens | |
| 2.4.2.4 | 2'-fluoro-3'-azido-2',3'-dideoxyuridine | N3FddU | Escherichia coli | |
| 2.4.2.4 | 2-(3,4-dichlorophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-(3,4-dihydroxyphenyl)quinazolin-4(3H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-(diphenylmethyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-phenyl-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-phenylquinazolin-4(3H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione | - |
Homo sapiens | |
| 2.4.2.4 | 2-[(3,4-dichlorophenyl)methyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-7-phenyl-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 3'-azidothymidine | AZT | Escherichia coli | |
| 2.4.2.4 | 3,3'-(1,3,4-oxadiazole-2,5-diyl)dipyridine | - |
Homo sapiens | |
| 2.4.2.4 | 3-(3-benzyl-2,4,5-trioxoimidazolidin-1-yl)propanamide | - |
Homo sapiens | |
| 2.4.2.4 | 3-benzyl-1H-2-benzopyran-1-one | - |
Homo sapiens | |
| 2.4.2.4 | 3-[(2-methoxy-6-nitroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione | - |
Homo sapiens | |
| 2.4.2.4 | 3-[(2-methylphenyl)methyl]-1H-2-benzopyran-1-one | - |
Homo sapiens | |
| 2.4.2.4 | 3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione | - |
Homo sapiens | |
| 2.4.2.4 | 3-[(E)-[(2,4-dichlorophenyl)imino]methyl]-4H-1-benzopyran-4-one | - |
Homo sapiens | |
| 2.4.2.4 | 3-[(E)-[(3-methoxy-4-methylphenyl)imino]methyl]-4H-1-benzopyran-4-one | - |
Homo sapiens | |
| 2.4.2.4 | 3-[2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]propanamide | - |
Homo sapiens | |
| 2.4.2.4 | 3-[3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]propanamide | - |
Homo sapiens | |
| 2.4.2.4 | 4-oxo-4H-1-benzopyran-3-carbaldehyde | - |
Homo sapiens | |
| 2.4.2.4 | 4-[(Z)-[(3-hydroxynaphthalen-2-yl)methylidene]amino]-1,5-dimethyl-2-phenylpyrazolidin-3-one | - |
Homo sapiens | |
| 2.4.2.4 | 5-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione | - |
Homo sapiens | |
| 2.4.2.4 | 5-(benzylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 5-(methylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 5-chloro-6-[([4-oxo-8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-2-yl]sulfanyl)methyl]pyrimidine-2,4(1H,3H)-dione | - |
Homo sapiens | |
| 2.4.2.4 | 5-phenyl-1,3,4-oxadiazole-2(3H)-thione | - |
Homo sapiens | |
| 2.4.2.4 | 5-[(E)-[2-(quinoxalin-2-yl)hydrazinylidene]methyl]benzene-1,2,4-triol | - |
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 | 6-aminothymine | - |
Escherichia coli | |
| 2.4.2.4 | 6-aminothymine | - |
Homo sapiens | |
| 2.4.2.4 | 7-(4-tert-butylphenyl)-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 7-(methylsulfanyl)-2-phenyl-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 7-deazaxanthine | - |
Escherichia coli | |
| 2.4.2.4 | 7-deazaxanthine | - |
Homo sapiens | |
| 2.4.2.4 | 7-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 7-phenylpyrazolo[1,5-a][1,3,5]triazine-2,4(1H,3H)-dione | - |
Homo sapiens | |
| 2.4.2.4 | 8-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | - |
Homo sapiens | |
| 2.4.2.4 | 8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | - |
Homo sapiens | |
| 2.4.2.4 | ethyl (3-benzyl-2,4,5-trioxoimidazolidin-1-yl)acetate | - |
Homo sapiens | |
| 2.4.2.4 | ethyl [2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]acetate | - |
Homo sapiens | |
| 2.4.2.4 | ethyl [3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetate | - |
Homo sapiens | |
| 2.4.2.4 | additional information | an array of structurally diverse non-nucleobase derivatives has beens designed, synthesized and established as promising TP inhibitors, structure-function analysis, overview | Escherichia coli | |
| 2.4.2.4 | additional information | an array of structurally diverse non-nucleobase derivatives has been designed, synthesized, and established as promising TP inhibitors, structure-function analysis, docking studies, overview. Analysis of oxadiazole and imidazolidine derivatives, pyrazolone and pyrazolo [1,5-a] [1,3,5]triazine analogues, 1,2,4-triazolo [1,5-a] [1,3,5]triazine analogues, quinazoline and quinoxaline derivatives, chromone and isocoumarin derivatives, and plant glycosides | Homo sapiens | |
| 2.4.2.4 | N-(4-oxo-2-sulfanylidene-8-[[4-(trifluoromethyl)phenyl]methyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea | - |
Homo sapiens | |
| 2.4.2.4 | N-(8-benzyl-4-oxo-2-sulfanylidene-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea | - |
Homo sapiens | |
| 2.4.2.4 | symplocomoside | - |
Homo sapiens | |
| 2.4.2.4 | symponoside | - |
Homo sapiens | |
| 2.4.2.4 | TFT | designated TAS-102 | Homo sapiens | |
| 2.4.2.4 | thymine | the substrate is a non-competitive inhibitor of the enzyme | Escherichia coli | |
| 2.4.2.4 | thymine | the substrate is a non-competitive inhibitor of the enzyme | Homo sapiens | |
| 2.4.2.4 | TP65 | - |
Escherichia coli | |
| 2.4.2.4 | TP65 | - |
Homo sapiens | |
| 2.4.2.4 | TPI | - |
Homo sapiens | |
| 2.4.2.4 | [2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]acetic acid | - |
Homo sapiens | |
| 2.4.2.4 | [3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetic acid | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.4.2.4 | thymidine + phosphate | Homo sapiens | - |
thymine + 2-deoxy-alpha-D-ribose 1-phosphate | - |
r | |
| 2.4.2.4 | thymine + 2-deoxy-alpha-D-ribose 1-phosphate | Escherichia coli | - |
thymidine + phosphate | - |
r | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 2.4.2.4 | Escherichia coli | P0C037 | - |
- |
| 2.4.2.4 | Homo sapiens | P19971 | - |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 2.4.2.4 | carcinoma cell | the enzyme is highly upregulated in a variety of solid tumours | Homo sapiens | - |
| 2.4.2.4 | endothelial cell | - |
Homo sapiens | - |
| 2.4.2.4 | additional information | thymidine phosphorylase (TP) expression is extremely low in healthy human tissues | Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.4.2.4 | thymidine + phosphate | - |
Homo sapiens | thymine + 2-deoxy-alpha-D-ribose 1-phosphate | - |
r | |
| 2.4.2.4 | thymine + 2-deoxy-alpha-D-ribose 1-phosphate | - |
Escherichia coli | thymidine + phosphate | - |
r | |
Subunits
| EC Number | Subunits | Comment | Organism |
|---|---|---|---|
| 2.4.2.4 | homodimer | 2 * 90000, SDS-PAGE | Escherichia coli |
| 2.4.2.4 | homodimer | 2 * 110000, SDS-PAGE | Homo sapiens |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 2.4.2.4 | 0.00004 | - |
pH and temperature not specified in the publication | Homo sapiens | 8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.00036 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-chloro-6-[([4-oxo-8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-2-yl]sulfanyl)methyl]pyrimidine-2,4(1H,3H)-dione | |
| 2.4.2.4 | 0.0015 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.0032 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-[(E)-[2-(quinoxalin-2-yl)hydrazinylidene]methyl]benzene-1,2,4-triol | |
| 2.4.2.4 | 0.00382 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-oxo-2-sulfanylidene-8-[[4-(trifluoromethyl)phenyl]methyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea | |
| 2.4.2.4 | 0.0066 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(4-tert-butylphenyl)-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.0097 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.01084 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(3,4-dichlorophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.013 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.013 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-[(3,4-dichlorophenyl)methyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.013 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-7-phenyl-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.0144 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[(2-methoxy-6-nitroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione | |
| 2.4.2.4 | 0.017 | - |
pH and temperature not specified in the publication | Homo sapiens | 6-amino-5-bromouracil | |
| 2.4.2.4 | 0.01977 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[(E)-[(3-methoxy-4-methylphenyl)imino]methyl]-4H-1-benzopyran-4-one | |
| 2.4.2.4 | 0.022 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-[(Z)-[(3-hydroxynaphthalen-2-yl)methylidene]amino]-1,5-dimethyl-2-phenylpyrazolidin-3-one | |
| 2.4.2.4 | 0.0263 | - |
pH and temperature not specified in the publication | Homo sapiens | 8-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.02992 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(8-benzyl-4-oxo-2-sulfanylidene-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea | |
| 2.4.2.4 | 0.035 | - |
pH and temperature not specified in the publication | Homo sapiens | TPI | |
| 2.4.2.4 | 0.03637 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(diphenylmethyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.037 | - |
pH and temperature not specified in the publication | Homo sapiens | 3,3'-(1,3,4-oxadiazole-2,5-diyl)dipyridine | |
| 2.4.2.4 | 0.03824 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione | |
| 2.4.2.4 | 0.03956 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.04 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-deazaxanthine | |
| 2.4.2.4 | 0.04 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]propanamide | |
| 2.4.2.4 | 0.04029 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[(E)-[(2,4-dichlorophenyl)imino]methyl]-4H-1-benzopyran-4-one | |
| 2.4.2.4 | 0.04061 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione | |
| 2.4.2.4 | 0.0429 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(3,4-dihydroxyphenyl)quinazolin-4(3H)-one | |
| 2.4.2.4 | 0.044 | - |
pH and temperature not specified in the publication | Homo sapiens | (2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one | |
| 2.4.2.4 | 0.0462 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-phenylquinazolin-4(3H)-one | |
| 2.4.2.4 | 0.0462 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one | |
| 2.4.2.4 | 0.05 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-phenyl-1,3,4-oxadiazole-2(3H)-thione | |
| 2.4.2.4 | 0.061 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[(2-methylphenyl)methyl]-1H-2-benzopyran-1-one | |
| 2.4.2.4 | 0.06545 | - |
pH and temperature not specified in the publication | Homo sapiens | symplocomoside | |
| 2.4.2.4 | 0.07 | - |
pH and temperature not specified in the publication | Homo sapiens | 6-aminothymine | |
| 2.4.2.4 | 0.085 | - |
pH and temperature not specified in the publication | Homo sapiens | [2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]acetic acid | |
| 2.4.2.4 | 0.088 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]propanamide | |
| 2.4.2.4 | 0.09505 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(methylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.103 | - |
pH and temperature not specified in the publication | Homo sapiens | 1-(2-phenylethyl)imidazolidine-2,4,5-trione | |
| 2.4.2.4 | 0.106 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(3-benzyl-2,4,5-trioxoimidazolidin-1-yl)propanamide | |
| 2.4.2.4 | 0.1112 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(benzylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one | |
| 2.4.2.4 | 0.115 | - |
pH and temperature not specified in the publication | Homo sapiens | 1-benzylimidazolidine-2,4,5-trione | |
| 2.4.2.4 | 0.128 | - |
pH and temperature not specified in the publication | Homo sapiens | 1-[(2-methylphenyl)methyl]imidazolidine-2,4,5-trione | |
| 2.4.2.4 | 0.22567 | - |
pH and temperature not specified in the publication | Homo sapiens | symponoside | |
| 2.4.2.4 | 0.236 | - |
pH and temperature not specified in the publication | Homo sapiens | [3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetic acid | |
| 2.4.2.4 | 0.264 | - |
pH and temperature not specified in the publication | Homo sapiens | (3-benzyl-2,4,5-trioxoimidazolidin-1-yl)acetic acid | |
| 2.4.2.4 | 0.303 | - |
pH and temperature not specified in the publication | Homo sapiens | ethyl [3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetate | |
| 2.4.2.4 | 0.342 | - |
pH and temperature not specified in the publication | Homo sapiens | ethyl (3-benzyl-2,4,5-trioxoimidazolidin-1-yl)acetate | |
| 2.4.2.4 | 0.357 | - |
pH and temperature not specified in the publication | Homo sapiens | ethyl [2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]acetate | |
Expression
| EC Number | Organism | Comment | Expression |
|---|---|---|---|
| 2.4.2.4 | Homo sapiens | the enzyme is highly upregulated in a variety of solid tumours | up |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 2.4.2.4 | evolution | the amino acid sequence of thymidine phosphorylase (TP) is extremely conserved. For instance, human TP shares 39% sequence identity with Escherichia coli TP | Homo sapiens |
| 2.4.2.4 | evolution | the amino acid sequence of thymidine phosphorylase (TP) is extremely conserved. For instance, human TP shares 39% sequence identity with Escherichia coli TP | Escherichia coli |
| 2.4.2.4 | metabolism | the intracellular catabolism of thymidine mediated via TP produces 2DDR-1P as a metabolic biproduct, which is subsequently converted to 2DDR by the nonenzymatic dephosphorylation. This 2DDR is then secreted from the cells to exhibit the angiogenic effects. Both TP and 2DDR directly stimulate the endothelial cell migration through the activation of focal adhesion kinase (FAK) and the formation of focal adhesions | Escherichia coli |
| 2.4.2.4 | metabolism | the intracellular catabolism of thymidine mediated via TP produces 2DDR-1P as a metabolic biproduct, which is subsequently converted to 2DDR by the nonenzymatic dephosphorylation. This 2DDR is then secreted from the cells to exhibit the angiogenic effects. Both TP and 2DDR directly stimulate the endothelial cell migration through the activation of focal adhesion kinase (FAK) and the formation of focal adhesions. TP and 2DDR roles in tumour development, overview | Homo sapiens |
| 2.4.2.4 | physiological function | thymidine phosphorylase (TP), an enzyme involved in pyrimidine salvage pathway, is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. The enzyme function in cancer development. TP activity is also shown to augment the levels of hypoxia-inducible factor (HIF)-1alpha during in vitro hypoxia in RT112 cells. Eventually, TP acts in concert with HIF-1a to induce VEGF secretion. Additionally, TP and VEGF are coexpressed in various human cancers and display a cooperative role in neovascularization. TP dramatically reduces the apoptotic index in various cancer cells. TP inactivates and eventually reduces the bioavailability of 5-trifluorothymidine (TFT), a clinically used anticancer drug | Homo sapiens |
| 2.4.2.4 | physiological function | thymidine phosphorylase (TP), an enzyme involved in pyrimidine salvage pathway, is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. TP activity is also shown to augment the levels of hypoxia-inducible factor (HIF)-1alpha during in vitro hypoxia in RT112 cells. Eventually, TP acts in concert with HIF-1a to induce VEGF secretion. Additionally, TP and VEGF are coexpressed in various human cancers and display a cooperative role in neovascularization. TP dramatically reduces the apoptotic index in various cancer cells | Escherichia coli |
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Release 2023.1 (January 2023)
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