Target Information

Target General Infomation
Target ID
T59929
Former ID
TTDR00251
Target Name
Thymidine phosphorylase
Gene Name
TYMP
Synonyms
Gliostatin; PD-ECGF; PDECGF; Platelet-derived endothelial cell growth factor; TP; TdRPase; TYMP
Target Type
Clinical Trial
Disease Depression [ICD9: 311; ICD10: F30-F39]
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.
BioChemical Class
Pentosyltransferase
Target Validation
T59929
UniProt ID
P19971
EC Number
EC 2.4.2.4
Sequence
MAALMTPGTGAPPAPGDFSGEGSQGLPDPSPEPKQLPELIRMKRDGGRLSEADIRGFVAA
VVNGSAQGAQIGAMLMAIRLRGMDLEETSVLTQALAQSGQQLEWPEAWRQQLVDKHSTGG
VGDKVSLVLAPALAACGCKVPMISGRGLGHTGGTLDKLESIPGFNVIQSPEQMQVLLDQA
GCCIVGQSEQLVPADGILYAARDVTATVDSLPLITASILSKKLVEGLSALVVDVKFGGAA
VFPNQEQARELAKTLVGVGASLGLRVAAALTAMDKPLGRCVGHALEVEEALLCMDGAGPP
DLRDLVTTLGGALLWLSGHAGTQAQGAARVAAALDDGSALGRFERMLAAQGVDPGLARAL
CSGSPAERRQLLPRAREQEELLAPADGTVELVRALPLALVLHELGAGRSRAGEPLRLGVG
AELLVDVGQRLRRGTPWLRVHRDGPALSGPQSRALQEALVLSDRAPFAAPSPFAELVLPP
QQ
Drugs and Mode of Action
Drug(s) Uridine Drug Info Approved Depression [467803], [521713]
Inhibitor 1-(cyclohexyl)methyl-5'-O-tritylinosine Drug Info [528407]
1-(cyclopropyl)methyl-5'-O-tritylinosine Drug Info [528407]
1-allyl-5'-O-tritylinosine Drug Info [528407]
1-benzyl-5'-O-tritylinosine Drug Info [528407]
1-propyl-5'-O-tritylinosine Drug Info [528407]
2'-aminoimidazolylmethyluracils Drug Info [535670]
5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione Drug Info [529120]
5-bromo-6-(cyclopropylamino)uracil hydrochloride Drug Info [527920]
5-bromo-6-hydrazinouracil hydrochloride Drug Info [527920]
5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione Drug Info [529120]
5-chloro-6-hydrazinouracil hydrochloride Drug Info [527920]
5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil Drug Info [530697]
6-amino-5-bromouracil Drug Info [529048]
6-amino-5-chlorouracil hydrochloride Drug Info [527920]
6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione Drug Info [529120]
Thymine Drug Info [551393]
Uridine Drug Info [536519]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Pyrimidine deoxyribonucleosides degradation
KEGG Pathway Pyrimidine metabolism
Drug metabolism - other enzymes
Metabolic pathways
Bladder cancer
NetPath Pathway TSH Signaling Pathway
PathWhiz Pathway Pyrimidine Metabolism
WikiPathways Bladder Cancer
Metabolism of nucleotides
Fluoropyrimidine Activity
References
Ref 467803(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 521713ClinicalTrials.gov (NCT00210080) A Study to Diagnose Lung Cancer by Sputum Cytology (01-312). U.S. National Institutes of Health.
Ref 527920Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. Epub 2005 Dec 5.Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
Ref 528407J Med Chem. 2006 Sep 7;49(18):5562-70.5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Ref 529048Eur J Med Chem. 2008 Jun;43(6):1248-60. Epub 2007 Aug 6.Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 530697Bioorg Med Chem Lett. 2010 Mar 1;20(5):1648-51. Epub 2010 Jan 21.The role of phosphate in the action of thymidine phosphorylase inhibitors: Implications for the catalytic mechanism.
Ref 535670Potential tumor-selective nitroimidazolylmethyluracil prodrug derivatives: inhibitors of the angiogenic enzyme thymidine phosphorylase. J Med Chem. 2003 Jan 16;46(2):207-9.
Ref 536519Enzymatic activities of uridine and thymidine phosphorylase in normal and cancerous uterine cervical tissues. Hum Cell. 2007 Nov;20(4):107-10.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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