Therapeutic Targets Database
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TTD Target ID: TTDS00056

Target Information
NameXanthine dehydrogenase/oxidase    
Type of targetSuccessful target    
SynonymsXanthine oxidase    
DiseaseGout
[ICD9: 274.00274.1274.8274.9   ICD10: M10]
[1]
Drug(s)AllopurinolApprovedHyperuricemia[2][3][4]
FebuxostatApprovedHyperuricaemia in patients with gout[5][6]
LeptinPhase IIIPrader-Willi Syndrome, Raynauds, Alzheimers, cardiovascular disease[7]
PathwayCaffeine metabolism
Drug metabolism - other enzymes
Metabolic pathways
Purine metabolism
UniProt IDP47989
PDB Structure2CKJ; 2E1Q.    
FunctionThis enzyme can be converted from the dehydrogenase form (d) to the oxidase form (o) irreversibly by proteolysis or reversibly through the oxidation of sulfhydryl groups.    
SequenceMTADKLVFFVNGRKVVEKNADPETTLLAYLRRKLGLSGTKLGCGEGGCGACTVMLSKYDR LQNKIVHFSANACLAPICSLHHVAVTTVEGIGSTKTRLHPVQERIAKSHGSQCGFCTPGI VMSMYTLLRNQPEPTMEEIENAFQGNLCRCTGYRPILQGFRTFARDGGCCGGDGNNPNCC MNQKKDHSVSLSPSLFKPEEFTPLDPTQEPIFPPELLRLKDTPRKQLRFEGERVTWIQAS TLKELLDLKAQHPDAKLVVGNTEIGIEMKFKNMLFPMIVCPAWIPELNSVEHGPDGISFG AACPLSIVEKTLVDAVAKLPAQKTEVFRGVLEQLRWFAGKQVKSVASVGGNIITASPISD LNPVFMASGAKLTLVSRGTRRTVQMDHTFFPGYRKTLLSPEEILLSIEIPYSREGEYFSA FKQASRREDDIAKVTSGMRVLFKPGTTEVQELALCYGGMANRTISALKTTQRQLSKLWKE ELLQDVCAGLAEELHLPPDAPGGMVDFRCTLTLSFFFKFYLTVLQKLGQENLEDKCGKLD PTFASATLLFQKDPPADVQLFQEVPKGQSEEDMVGRPLPHLAADMQASGEAVYCDDIPRY ENELSLRLVTSTRAHAKIKSIDTSEAKKVPGFVCFISADDVPGSNITGICNDETVFAKDK VTCVGHIIGAVVADTPEHTQRAAQGVKITYEELPAIITIEDAIKNNSFYGPELKIEKGDL KKGFSEADNVVSGEIYIGGQEHFYLETHCTIAVPKGEAGEMELFVSTQNTMKTQSFVAKM LGVPANRIVVRVKRMGGGFGGKETRSTVVSTAVALAAYKTGRPVRCMLDRDEDMLITGGR HPFLARYKVGFMKTGTVVALEVDHFSNVGNTQDLSQSIMERALFHMDNCYKIPNIRGTGR LCKTNLPSNTAFRGFGGPQGMLIAECWMSEVAVTCGMPAEEVRRKNLYKEGDLTHFNQKL EGFTLPRCWEECLASSQYHARKSEVDKFNKENCWKKRGLCIIPTKFGISFTVPFLNQAGA LLHVYTDGSVLLTHGGTEMGQGLHTKMVQVASRALKIPTSKIYISETSTNTVPNTSPTAA SVSADLNGQAVYAACQTILKRLEPYKKKNPSGSWEDWVTAAYMDTVSLSATGFYRTPNLG YSFETNSGNPFHYFSYGVACSEVEIDCLTGDHKNLRTDIVMDVGSSLNPAIDIGQVEGAF VQGLGLFTLEELHYSPEGSLHTRGPSTYKIPAFGSIPIEFRVSLLRDCPNKKAIYASKAV GEPPLFLAASIFFAIKDAIRAARAQHTGNNVKELFRLDSPATPEKIRNACVDKFTTLCVT GVPENCKPWSVRV
Related US Patent6,589,573
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1- (3-Cyano-phenyl)-1H-pyrazole-4-carboxylic acid[8]
2-chloro-6 (methylamino)purine[9]
3,4'- (1H-1,2,4-triazole-3,5-diyl)dipyridine[10]
3,5-bis (2-methylpyridin-4-yl)-1H-1,2,4-triazole[10]
3,5-di (pyridin-4-yl)-1H-1,2,4-triazole[10]
3-O-METHYLQUERCETIN[11]
ACACETIN[11]
AMENTOFLAVONE[11]
Allopurinol[2][3][4]
BAICALEIN[11]
CHRYSOERIOL[11]
CURCUMIN[12]
DIHYDROKAEMPFEROL[11]
FUKUGETIN[11]
Febuxostat[5][6]
Flavin-Adenine Dinucleotide[13]
LIQUIRTIGENIN[11]
Leptin[7]
PERSICARIN[11]
ROBINETIN[11]
SCUTELLAREIN[11]
WOGONIN[11]
Y-700[14]
dioxothiomolybdenum (VI) ion[15]
pentagalloyl glucose[16]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Prevention and management of gout. Drugs. 1993 Feb;45(2):212-22. To Reference
Ref 2Allopurinol: xanthine oxidase inhibitor. Tex Med. 1966 Jan;62(1):100-1. To Reference
Ref 3Purification, crystallization and preliminary X-ray diffraction studies of xanthine dehydrogenase and xanthine oxidase isolated from bovine milk. Acta Crystallogr D Biol Crystallogr. 2000 Dec;56(Pt 12):1656-8. To Reference
Ref 4Influence of postischemic administration of oxyradical antagonists on ischemic injury to rabbit skeletal muscle. Microsurgery. 1996;17(9):517-23. To Reference
Ref 5Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 6Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. To Reference
Ref 7Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. To Reference
Ref 8Bioorg Med Chem Lett. 2001 Apr 9;11(7):879-82.Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors. To Reference
Ref 9Bioorg Med Chem. 2007 May 15;15(10):3450-6. Epub 2007 Mar 12.The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors. To Reference
Ref 10Bioorg Med Chem Lett. 2009 Nov 1;19(21):6225-9. Epub 2009 Sep 2.Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected]. To Reference
Ref 11J. Nat. Prod. 51(2):345-348 (1988) To Reference
Ref 12J Nat Prod. 2009 Apr;72(4):725-31.Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin. To Reference
Ref 13Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 14Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 15Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 16J. Nat. Prod. 52(1):210-211 (1989) To Reference



 

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