Target Information

Target General Infomation
Target ID
T52389
Former ID
TTDC00200
Target Name
NAD(P)H dehydrogenase [quinone] 1
Gene Name
NQO1
Synonyms
Azoreductase; DT-diaphorase; DT-diaphorase 1; DTD; Menadione reductase; NAD(P)H:quinone oxidoreductase 1; Phylloqui reductase; Phylloquinone reductase; QR1; Qui reductase 1; Quinone reductase 1; NQO1
Target Type
Clinical Trial
Disease Huntington's disease [ICD9: 294.1, 333.4; ICD10: F02.2, G10]
Function
The 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 in prothrombin synthesis.
BioChemical Class
Oxidoreductases acting on NADH or NADPH
Target Validation
T52389
UniProt ID
P15559
EC Number
EC 1.6.5.2
Sequence
MVGRRALIVLAHSERTSFNYAMKEAAAAALKKKGWEVVESDLYAMNFNPIISRKDITGKL
KDPANFQYPAESVLAYKEGHLSPDIVAEQKKLEAADLVIFQFPLQWFGVPAILKGWFERV
FIGEFAYTYAAMYDKGPFRSKKAVLSITTGGSGSMYSLQGIHGDMNVILWPIQSGILHFC
GFQVLEPQLTYSIGHTPADARIQILEGWKKRLENIWDETPLYFAPSSLFDLNFQAGFLMK
KEVQDEEKNKKFGLSVGHHLGKSIPTDNQIKARK
Drugs and Mode of Action
Drug(s) Coenzyme Q10 analog Drug Info Phase 2 Huntington's disease [525079]
Inhibitor 2-Benzyl-1-hydroxy-3H-benzo[f]chromen-3-one Drug Info [530490]
3-(3,4-Dimethylbenzyl)-4-hydroxy-2H-chromen-2-one Drug Info [530490]
3-Benzyl-4-hydroxy-2H-benzo[h]chromen-2-one Drug Info [530490]
3-Benzyl-4-hydroxy-2H-chromen-2-one Drug Info [530490]
3-Benzyl-4-hydroxy-6,7-dimethyl-2H-chromen-2-one Drug Info [530490]
4-amino-2H-chromen-2-one Drug Info [529150]
4-Hydroxy-3-(1-naphthylmethyl)-2H-chromen-2-one Drug Info [530490]
4-Hydroxy-3-(2-naphthylmethyl)-2H-chromen-2-one Drug Info [530490]
Bishydroxy[2h-1-Benzopyran-2-One,1,2-Benzopyrone] Drug Info [551393]
Duroquinone Drug Info [551393]
ES-936 Drug Info [529109]
Ethyl Bis(4-hydroxy-2-oxo-2H-chromen-3-yl)acetate Drug Info [530490]
Flavin-Adenine Dinucleotide Drug Info [551393]
NSC-106080 Drug Info [531262]
NSC-106547 Drug Info [528457]
NSC-2113 Drug Info [528457]
NSC-224124 Drug Info [528457]
NSC-275420 Drug Info [528457]
NSC-316158 Drug Info [528457]
NSC-339580 Drug Info [528457]
NSC-339583 Drug Info [528457]
NSC-354279 Drug Info [528457]
NSC-621351 Drug Info [531262]
NSC-645808 Drug Info [528457]
NSC-645827 Drug Info [528457]
NSC-65069 Drug Info [531262]
NSC-73410 Drug Info [528457]
NSC-99528 Drug Info [531262]
Quinones Drug Info [535275]
Modulator Coenzyme Q10 analog Drug Info [544447]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Ubiquinone and other terpenoid-quinone biosynthesis
NetPath Pathway TCR Signaling Pathway
Pathway Interaction Database Validated transcriptional targets of TAp63 isoforms
PathWhiz Pathway Vitamin K Metabolism
WikiPathways Estrogen metabolism
Oxidative Stress
Transcriptional activation by NRF2
NRF2 pathway
Nuclear Receptors Meta-Pathway
Aryl Hydrocarbon Receptor Pathway
Apoptosis-related network due to altered Notch3 in ovarian cancer
Metabolism of amino acids and derivatives
Aryl Hydrocarbon Receptor
Dopamine metabolism
Arylhydrocarbon receptor (AhR) signaling pathway
References
Ref 525079ClinicalTrials.gov (NCT02352896) Long-Term Safety and Efficacy Evaluation of EPI-743 in Children With Leigh Syndrome. U.S. National Institutes of Health.
Ref 528457Bioorg Med Chem Lett. 2006 Dec 15;16(24):6246-54. Epub 2006 Sep 29.In silico identification and biochemical characterization of novel inhibitors of NQO1.
Ref 529109J Med Chem. 2007 Nov 15;50(23):5780-9. Epub 2007 Oct 18.Synthesis and evaluation of 3-aryloxymethyl-1,2-dimethylindole-4,7-diones as mechanism-based inhibitors of NAD(P)H:quinone oxidoreductase 1 (NQO1) activity.
Ref 529150J Med Chem. 2007 Dec 13;50(25):6316-25. Epub 2007 Nov 14.Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human pancreatic cancer toxicity.
Ref 530490J Med Chem. 2009 Nov 26;52(22):7142-56.Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: quinone oxidoreductase-1 (NQO1).
Ref 531262Bioorg 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 535275Structure-based development of anticancer drugs: complexes of NAD(P)H:quinone oxidoreductase 1 with chemotherapeutic quinones. Structure. 2001 Aug;9(8):659-67.
Ref 544447Therapeutic strategies for Leber's hereditary optic neuropathy: A current update. Intractable Rare Dis Res. 2013 November; 2(4): 130-135.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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