Target Information

Target General Infomation
Target ID
T75498
Former ID
TTDC00138
Target Name
NRH dehydrogenase [quinone] 2
Gene Name
NQO2
Synonyms
NAD(P)H qui oxidoreductase 2; NRH:qui oxidoreductase 2; NRH:quinone oxidoreductase 2; QR2; Qui reductase 2; Quinone oxidoreductase 2; Quinone reductase 2; NQO2
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinones involved in detoxification pathways as well as in biosynthetic processes such as the vitamin K-dependent gamma-carboxylation of glutamate residues in prothrombin synthesis.
BioChemical Class
Oxidoreductases acting on diphenols as donors
Target Validation
T75498
UniProt ID
P16083
EC Number
EC 1.10.99.2
Sequence
MAGKKVLIVYAHQEPKSFNGSLKNVAVDELSRQGCTVTVSDLYAMNLEPRATDKDITGTL
SNPEVFNYGVETHEAYKQRSLASDITDEQKKVREADLVIFQFPLYWFSVPAILKGWMDRV
LCQGFAFDIPGFYDSGLLQGKLALLSVTTGGTAEMYTKTGVNGDSRYFLWPLQHGTLHFC
GFKVLAPQISFAPEIASEEERKGMVAAWSQRLQTIWKEEPIPCTAHWHFGQ
Drugs and Mode of Action
Drug(s) NSC-645809 Drug Info Phase 2 Breast cancer [1]
Prolarix Drug Info Phase 2 Cancer [2]
CB1954 Drug Info Discontinued in Phase 2 Cancer [3]
Inhibitor 1,4-Dimethylquinolin-2(1H)-one Drug Info [4]
10-Propargyl-5,8-Dideazafolic Acid Drug Info [5]
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info [6]
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info [6]
5,6,8-Trimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info [4]
5,6,8-Trimethoxy-4-methylquinolin-2(1H)-one Drug Info [4]
5,8-dimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info [7]
5,8-Dimethoxy-4-methylquinolin-2(1H)-one Drug Info [4]
6,7,8-Trimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info [4]
6,7,8-Trimethoxy-4-methylquinolin-2(1H)-one Drug Info [4]
6,8-Dimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info [4]
6,8-Dimethoxy-4-methylquinolin-2(1H)-one Drug Info [4]
6-Methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one Drug Info [4]
7,8-Dimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info [4]
8-Methoxy-1,4-dimethylquinolin-2(1H)-one Drug Info [4]
CB1954 Drug Info [5]
Flavin-Adenine Dinucleotide Drug Info [5]
IODOMELATONIN Drug Info [4]
N-[2-(5-methoxy-1H-indol-3-yl)ethyl]acetamide Drug Info [7]
NSC-106080 Drug Info [8]
NSC-115890 Drug Info [8]
NSC-180969 Drug Info [8]
NSC-204996 Drug Info [8]
NSC-238146 Drug Info [8]
NSC-300853 Drug Info [8]
NSC-306843 Drug Info [8]
NSC-356819 Drug Info [8]
NSC-356820 Drug Info [8]
NSC-359466 Drug Info [8]
NSC-381864 Drug Info [8]
NSC-637991 Drug Info [9]
NSC-637992 Drug Info [9]
NSC-637993 Drug Info [9]
NSC-637994 Drug Info [9]
NSC-640353 Drug Info [8]
NSC-640556 Drug Info [8]
NSC-640558 Drug Info [8]
NSC-640559 Drug Info [8]
NSC-640566 Drug Info [8]
NSC-640583 Drug Info [8]
NSC-640584 Drug Info [8]
NSC-645808 Drug Info [9]
NSC-645809 Drug Info [9]
NSC-645811 Drug Info [9]
NSC-645812 Drug Info [9]
NSC-645831 Drug Info [9]
NSC-645833 Drug Info [9]
NSC-645834 Drug Info [9]
NSC-645835 Drug Info [9]
NSC-645836 Drug Info [9]
NSC-649091 Drug Info [8]
NSC-660838 Drug Info [9]
NSC-660839 Drug Info [9]
NSC-660840 Drug Info [9]
NSC-660841 Drug Info [9]
NSC-665126 Drug Info [8]
NSC-669977 Drug Info [8]
NSC-676468 Drug Info [8]
NSC-677939 Drug Info [8]
NSC-693571 Drug Info [8]
NSC-720622 Drug Info [8]
NSC-77833 Drug Info [8]
NSC-78017 Drug Info [8]
NSC-78021 Drug Info [8]
NSC-86715 Drug Info [8]
NSC-97374 Drug Info [8]
NSC-99495 Drug Info [8]
NSC-99528 Drug Info [8]
Prolarix Drug Info [10]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
REF 1Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10. Drug Metab Dispos. 2012 Sep;40(9):1736-43.
REF 2ClinicalTrials.gov (NCT00746590) Study of Anti-tumour Effects and Safety of Prolarix in Hepatocellular Carcinoma. U.S. National Institutes of Health.
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019051)
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.
REF 5How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 6Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer. Bioorg Med Chem. 2010 Jul 15;18(14):5352-66. doi: 10.1016/j.bmc.2010.05.042. Epub 2010 May 24.
REF 7The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
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).
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.
REF 10CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.

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