Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T59929
(Former ID: TTDR00251)
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| Target Name |
Thymidine phosphorylase (TYMP)
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| Synonyms |
TdRPase; TYMP; TP; Platelet-derived endothelial cell growth factor; PDECGF; PD-ECGF; Gliostatin
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| Gene Name |
TYMP
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| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Depression [ICD-11: 6A70-6A7Z] | |||||
| Function |
Catalyzes the reversible phosphorolysis of thymidine. The produced molecules are then utilized as carbon and energy sources or in the rescue of pyrimidine bases for nucleotide synthesis.
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| BioChemical Class |
Pentosyltransferase
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| UniProt ID | ||||||
| EC Number |
EC 2.4.2.4
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| Sequence |
MAALMTPGTGAPPAPGDFSGEGSQGLPDPSPEPKQLPELIRMKRDGGRLSEADIRGFVAA
VVNGSAQGAQIGAMLMAIRLRGMDLEETSVLTQALAQSGQQLEWPEAWRQQLVDKHSTGG VGDKVSLVLAPALAACGCKVPMISGRGLGHTGGTLDKLESIPGFNVIQSPEQMQVLLDQA GCCIVGQSEQLVPADGILYAARDVTATVDSLPLITASILSKKLVEGLSALVVDVKFGGAA VFPNQEQARELAKTLVGVGASLGLRVAAALTAMDKPLGRCVGHALEVEEALLCMDGAGPP DLRDLVTTLGGALLWLSGHAGTQAQGAARVAAALDDGSALGRFERMLAAQGVDPGLARAL CSGSPAERRQLLPRAREQEELLAPADGTVELVRALPLALVLHELGAGRSRAGEPLRLGVG AELLVDVGQRLRRGTPWLRVHRDGPALSGPQSRALQEALVLSDRAPFAAPSPFAELVLPP |
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Uridine | Drug Info | Approved | Depression | [2], [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 24 Inhibitor drugs | + | ||||
| 1 | Uridine | Drug Info | [1] | |||
| 2 | 1-(cyclohexyl)methyl-5'-O-tritylinosine | Drug Info | [4] | |||
| 3 | 1-(cyclopropyl)methyl-5'-O-tritylinosine | Drug Info | [4] | |||
| 4 | 1-allyl-5'-O-tritylinosine | Drug Info | [4] | |||
| 5 | 1-benzyl-5'-O-tritylinosine | Drug Info | [4] | |||
| 6 | 1-propyl-5'-O-tritylinosine | Drug Info | [4] | |||
| 7 | 2'-aminoimidazolylmethyluracils | Drug Info | [5] | |||
| 8 | 5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 9 | 5-bromo-6-(cyclopropylamino)uracil hydrochloride | Drug Info | [7] | |||
| 10 | 5-bromo-6-hydrazinouracil hydrochloride | Drug Info | [7] | |||
| 11 | 5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 12 | 5-chloro-6-hydrazinouracil hydrochloride | Drug Info | [7] | |||
| 13 | 5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil | Drug Info | [8] | |||
| 14 | 6-amino-5-bromouracil | Drug Info | [9] | |||
| 15 | 6-amino-5-chlorouracil hydrochloride | Drug Info | [7] | |||
| 16 | 6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 17 | 6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 18 | 6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 19 | 6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 20 | 6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 21 | 6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 22 | 6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 23 | 6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione | Drug Info | [6] | |||
| 24 | Thymine | Drug Info | [10] | |||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| BioCyc | [+] 1 BioCyc Pathways | + | ||||
| 1 | Pyrimidine deoxyribonucleosides degradation | |||||
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Pyrimidine metabolism | |||||
| 2 | Drug metabolism - other enzymes | |||||
| 3 | Metabolic pathways | |||||
| 4 | Bladder cancer | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | TSH Signaling Pathway | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Pyrimidine Metabolism | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Bladder Cancer | |||||
| 2 | Metabolism of nucleotides | |||||
| 3 | Fluoropyrimidine Activity | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Enzymatic activities of uridine and thymidine phosphorylase in normal and cancerous uterine cervical tissues. Hum Cell. 2007 Nov;20(4):107-10. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4566). | |||||
| REF 3 | ClinicalTrials.gov (NCT00210080) A Study to Diagnose Lung Cancer by Sputum Cytology (01-312). U.S. National Institutes of Health. | |||||
| REF 4 | 5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase. J Med Chem. 2006 Sep 7;49(18):5562-70. | |||||
| REF 5 | Potential tumor-selective nitroimidazolylmethyluracil prodrug derivatives: inhibitors of the angiogenic enzyme thymidine phosphorylase. J Med Chem. 2003 Jan 16;46(2):207-9. | |||||
| REF 6 | Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase. J Med Chem. 2007 Nov 29;50(24):6016-23. | |||||
| REF 7 | Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. | |||||
| REF 8 | The role of phosphate in the action of thymidine phosphorylase inhibitors: Implications for the catalytic mechanism. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1648-51. | |||||
| REF 9 | Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors. Eur J Med Chem. 2008 Jun;43(6):1248-60. | |||||
| REF 10 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
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