Therapeutic Targets Database
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TTD Target ID: TTDC00138

Target Information
NameNRH dehydrogenase [quinone] 2    
Type of targetClinical trial target    
SynonymsNAD(P)H qui oxidoreductase 2    
NQO2    
NRH:qui oxidoreductase 2    
NRH:quinone oxidoreductase 2    
QR2    
Qui reductase 2    
Quinone oxidoreductase 2    
Quinone reductase 2    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Malaria
[ICD9: 084   ICD10: B50-B54]
[2]
Tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[3]
Drug(s)CB1954/EP-0152R, NQO2 prodrug therapyPhase ICancer/Tumors[1]
ProlarixTerminated in Phase ICancer/Tumors[1]
BioChemical ClassOxidoreductases acting on diphenols as donors    
EC NumberEC 1.6.99.-
EC 1.6.99.2
UniProt IDP16083
Q6LFA2
PDB Structure1QR2; 1SG0; 1XI2; 1ZX1; 2BZS; 2QMY; 2QMZ; 2QR2; 2QWX; 2QX4; 2QX6; 2QX8; 2QX9; 3FW1; 3G5M; 3GAM; 3NFR; 3NHF; 3NHJ; 3NHK; 3NHL; 3NHP; 3NHR; 3NHS; 3NHU; 3NHW; 3NHY; 3O2N; 3O73; 3OVM; 3OWH; 3OWX; 3OX1; 3OX2; 3OX3; 3TE7; 3TEM; 3TZB; 3UXE; 3UXH; 4FGJ; 4FGK; 4FGL.    
FunctionThe enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinons involved in detoxification pathways as well as in biosynthetic processes such as the vitamin k-dependent gamma-carboxylation of glutamate residues.    
SequenceMICVKNILKRYKNSPLNELRNNRKYYEGSFVKSIKFSTSNYGSNEKKPNDIEKNKNVSIN LNEGNILQSEIYDTVVIGGGVTGTALFFLLSKFTNLKKLAIIERRDNFALVASHGKNNSQ TIHCGDIETNYSFEKAKFIKRYADMLRNYLTNIPKEKRENISSVTQKMVLGVGEKECQFL EERYPVFRQLFNSMKLYNKDDIHEVEPRVALKDSHTLREEQLSALYMPPELTTCDYQKLS ESFIESARTVPNKTISINLLTEVINIEEVNDSLYKIHTNKGIINSRFVVVCACGHSLMIA QKMNYGLEYSCMPVAGSFYFTDNILKGKVYTIQNPALPFAAVHGDPDIIEKGKTRFGPTA IPLPLLERDNIKTLLDFLKVWNPDLSLFQVYYNLFKDMTMLKYVARNVLFEIPVLNKYLF LKDVKKIIPSLTIKDLTYCVGYGGVRPQLINKKSKKLILGEGKIDPGKNIIFNITPSPGA TTCLGNGEFDMNTICERLNAKINKNDVKKYLYEGEYPVNYL
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,4-Dimethylquinolin-2 (1H)-one[4]
10-Propargyl-5,8-Dideazafolic Acid[5]
3,4,5-Trimethoxy-4'-amino-trans-stilbene[6]
3,5-Dimethoxy-4'-amino-trans-stilbene[6]
5,6,8-Trimethoxy-1,4-dimethylquinolin-2 (1H)-one[4]
5,6,8-Trimethoxy-4-methylquinolin-2 (1H)-one[4]
5,8-Dimethoxy-4-methylquinolin-2 (1H)-one[4]
5,8-dimethoxy-1,4-dimethylquinolin-2 (1H)-one[7]
6,7,8-Trimethoxy-1,4-dimethylquinolin-2 (1H)-one[4]
6,7,8-Trimethoxy-4-methylquinolin-2 (1H)-one[4]
6,8-Dimethoxy-1,4-dimethylquinolin-2 (1H)-one[4]
6,8-Dimethoxy-4-methylquinolin-2 (1H)-one[4]
6-Methyl-[1,3]dioxolo[4,5-h]quinolin-8 (9H)-one[4]
7,8-Dimethoxy-1,4-dimethylquinolin-2 (1H)-one[4]
8-Methoxy-1,4-dimethylquinolin-2 (1H)-one[4]
CB1954[5]
CB1954/EP-0152R, NQO2 prodrug therapy[1]
Flavin-Adenine Dinucleotide[5]
IODOMELATONIN[4]
N-[2- (5-methoxy-1H-indol-3-yl)ethyl]acetamide[7]
NSC-106080[8]
NSC-115890[8]
NSC-180969[8]
NSC-204996[8]
NSC-238146[8]
NSC-300853[8]
NSC-306843[8]
NSC-356819[8]
NSC-356820[8]
NSC-359466[8]
NSC-381864[8]
NSC-637991[9]
NSC-637992[9]
NSC-637993[9]
NSC-637994[9]
NSC-640353[8]
NSC-640556[8]
NSC-640558[8]
NSC-640559[8]
NSC-640566[8]
NSC-640583[8]
NSC-640584[8]
NSC-645808[9]
NSC-645809[9]
NSC-645811[9]
NSC-645812[9]
NSC-645831[9]
NSC-645833[9]
NSC-645834[9]
NSC-645835[9]
NSC-645836[9]
NSC-649091[8]
NSC-660838[9]
NSC-660839[9]
NSC-660840[9]
NSC-660841[9]
NSC-665126[8]
NSC-669977[8]
NSC-676468[8]
NSC-677939[8]
NSC-693571[8]
NSC-720622[8]
NSC-77833[8]
NSC-78017[8]
NSC-78021[8]
NSC-86715[8]
NSC-97374[8]
NSC-99495[8]
NSC-99528[8]
Resveratrol[10]
ActivatorProlarix[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 2Kinetic mechanism of quinone oxidoreductase 2 and its inhibition by the antimalarial quinolines. Biochemistry. 2004 Apr 20;43(15):4538-47. To Reference
Ref 3Bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy. Cancer Res. 2000 Aug 1;60(15):4179-86. To Reference
Ref 4J Med Chem. 2009 Apr 9;52(7):1873-84.Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities. To Reference
Ref 5Overington 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 6Bioorg. Med. Chem. 18(14):5352-5366 (2010) To Reference
Ref 7Berman 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 8Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 9Bioorg Med Chem Lett. 2010 May 1;20(9):2832-6. Epub 2010 Mar 15.Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2. To Reference
Ref 10Farina A, Ferranti C, Marra C: An improved synthesis of resveratrol. Nat Prod Res. 2006 Mar;20(3):247-52. To Reference



 

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