Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM9QU5Y)

• Drug Name: GSK343 Drug Info
• Synonyms: compound 6 [PMID 24900432]; GSK 343

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 71268957
  CAS Number: CAS 1346704-33-3
  TTD Drug ID: DM9QU5Y

Molecule-Related Drug Atlas

Drug(s) Targeting Enhancer of zeste homolog 1 (EZH1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DS-3201b	DMI69E5	T-cell leukaemia	2A90	Phase 2	[4]
DS-3201	DMRLPFG	Acute lymphoblastic leukaemia	2A85	Phase 1	[5]
HH2853	DMQIE58	Non-hodgkin lymphoma	2B33.5	Phase 1	[6]

Drug(s) Targeting Enhancer of zeste homolog 2 (EZH2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tazemetostat	DMWP1BH	Follicular lymphoma	2A80	Approved	[7]
DS-3201b	DMI69E5	T-cell leukaemia	2A90	Phase 2	[4]
CPI-1205	DM3XWJ8	Prostate cancer	2C82.0	Phase 1/2	[5]
SHR2554	DMMUCH0	Prostate cancer	2C82.0	Phase 1/2	[8]
CPI-0209	DMJEXLI	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
DS-3201	DMRLPFG	Acute lymphoblastic leukaemia	2A85	Phase 1	[5]
HH2853	DMQIE58	Non-hodgkin lymphoma	2B33.5	Phase 1	[6]
GSK2816126	DMJDVW4	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
PF-06821497	DML3WT6	Diffuse large B-cell lymphoma	2A81	Phase 1	[11]
PMID28394193-Compound-56	DMQRFZK	N. A.	N. A.	Patented	[12]

Drug(s) Affected By Histone-lysine N-methyltransferase EZH2 (EZH2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[13]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[14]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[15]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[16]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[17]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[18]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[19]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[20]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[20]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[21]

Drug(s) Affected By Endoribonuclease Dicer (DICER1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selenium	DM25CGV	N. A.	N. A.	Approved	[22]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[23]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[24]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[25]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[26]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[27]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[28]
Amphotericin B	DMTAJQE	Acne vulgaris	ED80	Approved	[29]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[30]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[31]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Enhancer of zeste homolog 1 (EZH1)	TTNJA0C	EZH1_HUMAN	Inhibitor	[1]
Enhancer of zeste homolog 2 (EZH2)	TT9MZCQ	EZH2_HUMAN	Inhibitor	[1]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Endoribonuclease Dicer (DICER1)	OTTVSEY0	DICER_HUMAN	Gene/Protein Processing	[2]
Histone-lysine N-methyltransferase EZH2 (EZH2)	OTIEHTKW	EZH2_HUMAN	Gene/Protein Processing	[3]

References

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• [3] Three-dimensional culture sensitizes epithelial ovarian cancer cells to EZH2 methyltransferase inhibition. Cell Cycle. 2013 Jul 1;12(13):2113-9. doi: 10.4161/cc.25163. Epub 2013 Jun 10.
• [4] Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] Clinical pipeline report, company report or official report of HaiHe Biopharma.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
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• [9] ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
• [10] National Cancer Institute Drug Dictionary (drug id 756211).
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• [21] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [22] Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
• [23] Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
• [24] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [25] Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
• [26] miR-148a/LDLR mediates hypercholesterolemia induced by prenatal dexamethasone exposure in male offspring rats. Toxicol Appl Pharmacol. 2020 May 15;395:114979. doi: 10.1016/j.taap.2020.114979. Epub 2020 Mar 29.
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• [28] Low doses of cisplatin induce gene alterations, cell cycle arrest, and apoptosis in human promyelocytic leukemia cells. Biomark Insights. 2016 Aug 24;11:113-21.
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