Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJLP0R)

• DTT Name: Quinone reductase 2 (NQO2)
• Synonyms: Quinone oxidoreductase 2; Qui reductase 2; QR2; NRH:quinone oxidoreductase 2; NRH:qui oxidoreductase 2; NQO2; NAD(P)H qui oxidoreductase 2
• Gene Name: NQO2
• DTT Type: Successful target; [1]
• Related Disease: Insomnia [ICD-11: 7A00-7A0Z]
• BioChemical Class: Diphenol donor oxidoreductase
• UniProt ID: NQO2_HUMAN
• TTD ID: T75498
• EC Number: EC 1.10.5.1
• Sequence:
  MAGKKVLIVYAHQEPKSFNGSLKNVAVDELSRQGCTVTVSDLYAMNLEPRATDKDITGTL
  SNPEVFNYGVETHEAYKQRSLASDITDEQKKVREADLVIFQFPLYWFSVPAILKGWMDRV
  LCQGFAFDIPGFYDSGLLQGKLALLSVTTGGTAEMYTKTGVNGDSRYFLWPLQHGTLHFC
  GFKVLAPQISFAPEIASEEERKGMVAAWSQRLQTIWKEEPIPCTAHWHFGQ
• 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.
• Reactome Pathway: Phase I - Functionalization of compounds (R-HSA-211945)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Melatonin	DMKWFBT	Insomnia	7A00-7A0Z	Approved	[1]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NSC-645809	DMPJQZG	Breast cancer	2C60-2C65	Phase 2	[2]
Prolarix	DMZIQ8G	Solid tumour/cancer	2A00-2F9Z	Phase 2	[3]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CB1954	DMVP4YK	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[4]

65 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,4-Dimethylquinolin-2(1H)-one	DMRT13B	Discovery agent	N.A.	Investigative	[5]
10-Propargyl-5,8-Dideazafolic Acid	DMR3A5N	N. A.	N. A.	Investigative	[4]
2-iodo-melatonin	DMSEIUP	Discovery agent	N.A.	Investigative	[5]
3,4,5-Trimethoxy-4'-amino-trans-stilbene	DMDBOJ5	Discovery agent	N.A.	Investigative	[6]
3,5-Dimethoxy-4'-amino-trans-stilbene	DMC3917	Discovery agent	N.A.	Investigative	[6]
5,6,8-Trimethoxy-1,4-dimethylquinolin-2(1H)-one	DMNHT7Q	Discovery agent	N.A.	Investigative	[5]
5,6,8-Trimethoxy-4-methylquinolin-2(1H)-one	DM97XZ1	Discovery agent	N.A.	Investigative	[5]
5,8-dimethoxy-1,4-dimethylquinolin-2(1H)-one	DMJ1IRO	Discovery agent	N.A.	Investigative	[1]
5,8-Dimethoxy-4-methylquinolin-2(1H)-one	DMEMBKW	Discovery agent	N.A.	Investigative	[5]
6,7,8-Trimethoxy-1,4-dimethylquinolin-2(1H)-one	DMAMD87	Discovery agent	N.A.	Investigative	[5]
6,7,8-Trimethoxy-4-methylquinolin-2(1H)-one	DMJX9NQ	Discovery agent	N.A.	Investigative	[5]
6,8-Dimethoxy-1,4-dimethylquinolin-2(1H)-one	DMAFP18	Discovery agent	N.A.	Investigative	[5]
6,8-Dimethoxy-4-methylquinolin-2(1H)-one	DMYKSTZ	Discovery agent	N.A.	Investigative	[5]
6-Methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one	DMOIC64	Discovery agent	N.A.	Investigative	[5]
7,8-Dimethoxy-1,4-dimethylquinolin-2(1H)-one	DMPF6MD	Discovery agent	N.A.	Investigative	[5]
8-Methoxy-1,4-dimethylquinolin-2(1H)-one	DM0Y52J	Discovery agent	N.A.	Investigative	[5]
Decynium 22	DMWCTZ7	Discovery agent	N.A.	Investigative	[7]
Flavin-Adenine Dinucleotide	DM5S4GK	Discovery agent	N.A.	Investigative	[4]
NSC-106080	DMR6P9S	Discovery agent	N.A.	Investigative	[7]
NSC-115890	DMPLUHT	Discovery agent	N.A.	Investigative	[7]
NSC-180969	DMZFHL0	Discovery agent	N.A.	Investigative	[7]
NSC-204996	DMAQGIW	Discovery agent	N.A.	Investigative	[7]
NSC-238146	DMWXNOI	Discovery agent	N.A.	Investigative	[7]
NSC-300853	DM6IF8N	Discovery agent	N.A.	Investigative	[7]
NSC-306843	DMZYJU0	Discovery agent	N.A.	Investigative	[7]
NSC-356819	DMXT1EK	Discovery agent	N.A.	Investigative	[7]
NSC-356820	DM9CM5V	Discovery agent	N.A.	Investigative	[7]
NSC-359466	DMHUG1W	Discovery agent	N.A.	Investigative	[7]
NSC-381864	DMLGWHM	Discovery agent	N.A.	Investigative	[7]
NSC-637991	DMY7EAF	Discovery agent	N.A.	Investigative	[2]
NSC-637992	DM0U7CK	Discovery agent	N.A.	Investigative	[2]
NSC-637993	DM2HC8L	Discovery agent	N.A.	Investigative	[2]
NSC-637994	DMKA8YT	Discovery agent	N.A.	Investigative	[2]
NSC-640353	DMZCYM1	Discovery agent	N.A.	Investigative	[7]
NSC-640556	DM3DW6A	Discovery agent	N.A.	Investigative	[7]
NSC-640558	DMPFC5U	Discovery agent	N.A.	Investigative	[7]
NSC-640559	DMMT73G	Discovery agent	N.A.	Investigative	[7]
NSC-640566	DMSJ06G	Discovery agent	N.A.	Investigative	[7]
NSC-640583	DMC4Y0R	Discovery agent	N.A.	Investigative	[7]
NSC-640584	DMY2API	Discovery agent	N.A.	Investigative	[7]
NSC-645808	DMMBAR3	Discovery agent	N.A.	Investigative	[2]
NSC-645811	DMCNIT2	Discovery agent	N.A.	Investigative	[2]
NSC-645812	DM1MPJ9	Discovery agent	N.A.	Investigative	[2]
NSC-645831	DMSO215	Discovery agent	N.A.	Investigative	[2]
NSC-645833	DM1AD8T	Discovery agent	N.A.	Investigative	[2]
NSC-645834	DMY5JFB	Discovery agent	N.A.	Investigative	[2]
NSC-645835	DMKDVP7	Discovery agent	N.A.	Investigative	[2]
NSC-645836	DMQ13SI	Discovery agent	N.A.	Investigative	[2]
NSC-649091	DM6F3HV	Discovery agent	N.A.	Investigative	[7]
NSC-660838	DMXDNQ6	Discovery agent	N.A.	Investigative	[2]
NSC-660839	DM8LOCA	Discovery agent	N.A.	Investigative	[2]
NSC-660840	DMB5PLD	Discovery agent	N.A.	Investigative	[2]
NSC-660841	DMXHPV0	Discovery agent	N.A.	Investigative	[2]
NSC-665126	DMNQXE0	Discovery agent	N.A.	Investigative	[7]
NSC-669977	DMVFZKQ	Discovery agent	N.A.	Investigative	[7]
NSC-676468	DMY4MPG	Discovery agent	N.A.	Investigative	[7]
NSC-677939	DM35V46	Discovery agent	N.A.	Investigative	[7]
NSC-693571	DMKMTJ9	Discovery agent	N.A.	Investigative	[7]
NSC-720622	DMCP1I6	Discovery agent	N.A.	Investigative	[7]
NSC-77833	DM82XAU	Discovery agent	N.A.	Investigative	[7]
NSC-78017	DM8R12J	Discovery agent	N.A.	Investigative	[7]
NSC-78021	DM7L3DE	Discovery agent	N.A.	Investigative	[7]
NSC-86715	DMA53YD	Discovery agent	N.A.	Investigative	[7]
NSC-99495	DM96X2U	Discovery agent	N.A.	Investigative	[7]
NSC-99528	DMXZAIG	Discovery agent	N.A.	Investigative	[7]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Breast cancer	2C82	Breast tissue	1.56E-10	-0.13	-0.34

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: Quinone reductase 2 (NQO2) DME Info
• Gene Name: NQO2

1 Clinical Trial Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nicotinamide riboside	DMJBYSE	Mitochondrial myopathy	8C73	Phase 1	[8]

References

• [1] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [2] Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2. Bioorg Med Chem Lett. 2010 May 1;20(9):2832-6.
• [3] CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
• [4] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [5] Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities. J Med Chem. 2009 Apr 9;52(7):1873-84.
• [6] Design, 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.
• [7] 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.
• [8] Insights into the redox cycle of human quinone reductase 2. Free Radic Res. 2011 Oct;45(10):1184-95.