Target General Infomation
Target ID
T52389 (Former ID: TTDC00200)
Target Name
Quinone reductase 1 (NQO1)
Synonyms
Qui reductase 1; QR1; Phylloquinone reductase; Phylloqui reductase; NMOR1; NAD(P)H:quinone oxidoreductase 1; NAD(P)H dehydrogenase [quinone] 1; Menadione reductase; DTD; DT-diaphorase 1; DT-diaphorase; DIA4; Azoreductase
Gene Name
NQO1
Target Type
Clinical trial target
[1]
Disease [+] 6 Target-related Diseases +
1 Choreiform disorder [ICD-11: 8A01]
2 CNS anomalies syndrome [ICD-11: LD20]
3 Inborn energy metabolism error [ICD-11: 5C53]
4 Intellectual development disorder [ICD-11: LD90]
5 Pancreatic cancer [ICD-11: 2C10]
6 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
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
NADH/NADPH oxidoreductase
UniProt ID
NQO1_HUMAN
EC Number
EC 1.6.5.2
Sequence
MVGRRALIVLAHSERTSFNYAMKEAAAAALKKKGWEVVESDLYAMNFNPIISRKDITGKL
KDPANFQYPAESVLAYKEGHLSPDIVAEQKKLEAADLVIFQFPLQWFGVPAILKGWFERV
FIGEFAYTYAAMYDKGPFRSKKAVLSITTGGSGSMYSLQGIHGDMNVILWPIQSGILHFC
GFQVLEPQLTYSIGHTPADARIQILEGWKKRLENIWDETPLYFAPSSLFDLNFQAGFLMK
KEVQDEEKNKKFGLSVGHHLGKSIPTDNQIKARK
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 3 Clinical Trial Drugs +
1 ARQ 761 Drug Info Phase 2 Pancreatic cancer [2]
2 BioE-743 Drug Info Phase 2 Leigh syndrome [3]
3 Coenzyme Q10 analog Drug Info Phase 2 Huntington disease [4]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 30 Inhibitor drugs +
1 ARQ 761 Drug Info [2]
2 2-Benzyl-1-hydroxy-3H-benzo[f]chromen-3-one Drug Info [5]
3 3-(3,4-Dimethylbenzyl)-4-hydroxy-2H-chromen-2-one Drug Info [5]
4 3-Benzyl-4-hydroxy-2H-benzo[h]chromen-2-one Drug Info [5]
5 3-Benzyl-4-hydroxy-2H-chromen-2-one Drug Info [5]
6 3-Benzyl-4-hydroxy-6,7-dimethyl-2H-chromen-2-one Drug Info [5]
7 4-amino-2H-chromen-2-one Drug Info [6]
8 4-Hydroxy-3-(1-naphthylmethyl)-2H-chromen-2-one Drug Info [5]
9 4-Hydroxy-3-(2-naphthylmethyl)-2H-chromen-2-one Drug Info [5]
10 Bishydroxy[2h-1-Benzopyran-2-One,1,2-Benzopyrone] Drug Info [7]
11 Duroquinone Drug Info [7]
12 ES-936 Drug Info [8]
13 Ethyl Bis(4-hydroxy-2-oxo-2H-chromen-3-yl)acetate Drug Info [5]
14 Flavin-Adenine Dinucleotide Drug Info [7]
15 NSC-106080 Drug Info [9]
16 NSC-106547 Drug Info [10]
17 NSC-2113 Drug Info [10]
18 NSC-224124 Drug Info [10]
19 NSC-275420 Drug Info [10]
20 NSC-316158 Drug Info [10]
21 NSC-339580 Drug Info [10]
22 NSC-339583 Drug Info [10]
23 NSC-354279 Drug Info [10]
24 NSC-621351 Drug Info [9]
25 NSC-645808 Drug Info [10]
26 NSC-645827 Drug Info [10]
27 NSC-65069 Drug Info [9]
28 NSC-73410 Drug Info [10]
29 NSC-99528 Drug Info [9]
30 Quinones Drug Info [11]
Modulator [+] 2 Modulator drugs +
1 BioE-743 Drug Info [3]
2 Coenzyme Q10 analog Drug Info [1]
Target Regulators
Target-regulating Transcription Factors
Target-interacting Proteins
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 1 KEGG Pathways +
1 Ubiquinone and other terpenoid-quinone biosynthesis
NetPath Pathway [+] 1 NetPath Pathways +
1 TCR Signaling Pathway
Pathwhiz Pathway [+] 1 Pathwhiz Pathways +
1 Vitamin K Metabolism
PID Pathway [+] 1 PID Pathways +
1 Validated transcriptional targets of TAp63 isoforms
WikiPathways [+] 11 WikiPathways +
1 Estrogen metabolism
2 Oxidative Stress
3 Transcriptional activation by NRF2
4 NRF2 pathway
5 Nuclear Receptors Meta-Pathway
6 Aryl Hydrocarbon Receptor Pathway
7 Apoptosis-related network due to altered Notch3 in ovarian cancer
8 Metabolism of amino acids and derivatives
9 Aryl Hydrocarbon Receptor
10 Dopamine metabolism
11 Arylhydrocarbon receptor (AhR) signaling pathway
Target-Related Models and Studies
Target Validation
References
REF 1 Therapeutic strategies for Leber's hereditary optic neuropathy: A current update. Intractable Rare Dis Res. 2013 November; 2(4): 130-135.
REF 2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 4 ClinicalTrials.gov (NCT02352896) Long-Term Safety and Efficacy Evaluation of EPI-743 in Children With Leigh Syndrome. U.S. National Institutes of Health.
REF 5 Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: quinone oxidoreductase-1 (NQO1). J Med Chem. 2009 Nov 26;52(22):7142-56.
REF 6 Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human panc... J Med Chem. 2007 Dec 13;50(25):6316-25.
REF 7 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 8 Synthesis and evaluation of 3-aryloxymethyl-1,2-dimethylindole-4,7-diones as mechanism-based inhibitors of NAD(P)H:quinone oxidoreductase 1 (NQO1) ... J Med Chem. 2007 Nov 15;50(23):5780-9.
REF 9 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
REF 10 In silico identification and biochemical characterization of novel inhibitors of NQO1. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6246-54.
REF 11 Structure-based development of anticancer drugs: complexes of NAD(P)H:quinone oxidoreductase 1 with chemotherapeutic quinones. Structure. 2001 Aug;9(8):659-67.

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