Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT4LVGDN)

• DOT Name: Protein C-ets-1 (ETS1)
• Synonyms: p54
• Gene Name: ETS1
• Related Disease:
  Congenital heart disease
  Tourette syndrome
• UniProt ID: ETS1_HUMAN
• PDB ID: 1GVJ; 2NNY; 2STT; 2STW; 3MFK; 3RI4; 3WTS; 3WTT; 3WTU; 3WTV; 3WTW; 3WTX; 3WTY; 3WTZ; 3WU0; 3WU1; 4L0Y; 4L0Z; 4L18; 4LG0; 5ZMC
• Pfam ID: PF00178 ; PF19525 ; PF02198
• Sequence:
  MKAAVDLKPTLTIIKTEKVDLELFPSPDMECADVPLLTPSSKEMMSQALKATFSGFTKEQ
  QRLGIPKDPRQWTETHVRDWVMWAVNEFSLKGVDFQKFCMNGAALCALGKDCFLELAPDF
  VGDILWEHLEILQKEDVKPYQVNGVNPAYPESRYTSDYFISYGIEHAQCVPPSEFSEPSF
  ITESYQTLHPISSEELLSLKYENDYPSVILRDPLQTDTLQNDYFAIKQEVVTPDNMCMGR
  TSRGKLGGQDSFESIESYDSCDRLTQSWSSQSSFNSLQRVPSYDSFDSEDYPAALPNHKP
  KGTFKDYVRDRADLNKDKPVIPAAALAGYTGSGPIQLWQFLLELLTDKSCQSFISWTGDG
  WEFKLSDPDEVARRWGKRKNKPKMNYEKLSRGLRYYYDKNIIHKTAGKRYVYRFVCDLQS
  LLGYTPEELHAMLDVKPDADE
• Function: Transcription factor. Directly controls the expression of cytokine and chemokine genes in a wide variety of different cellular contexts. May control the differentiation, survival and proliferation of lymphoid cells. May also regulate angiogenesis through regulation of expression of genes controlling endothelial cell migration and invasion ; [Isoform Ets-1 p27]: Acts as a dominant-negative for isoform c-ETS-1A.
• Tissue Specificity: Highly expressed within lymphoid cells. Isoforms c-ETS-1A and Ets-1 p27 are both detected in all fetal tissues tested, but vary with tissue type in adult tissues. None is detected in brain or kidney.
• KEGG Pathway:
  Ras sig.ling pathway (hsa04014)
  Cellular senescence (hsa04218)
  Human T-cell leukemia virus 1 infection (hsa05166)
  Pathways in cancer (hsa05200)
  Re.l cell carcinoma (hsa05211)
• Reactome Pathway: Oncogene Induced Senescence (R-HSA-2559585)

Molecular Interaction Atlas (MIA) of This DOT

2 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Congenital heart disease	DISQBA23	Moderate	Autosomal dominant	[1]
Tourette syndrome	DISX9D54	No Known	Unknown	[2]

3 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the methylation of Protein C-ets-1 (ETS1).	[3]
TAK-243	DM4GKV2	Phase 1	TAK-243 increases the sumoylation of Protein C-ets-1 (ETS1).	[21]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the methylation of Protein C-ets-1 (ETS1).	[23]

26 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Protein C-ets-1 (ETS1).	[4]
Tretinoin	DM49DUI	Approved	Tretinoin increases the expression of Protein C-ets-1 (ETS1).	[5]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Protein C-ets-1 (ETS1).	[6]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Protein C-ets-1 (ETS1).	[7]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of Protein C-ets-1 (ETS1).	[8]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Protein C-ets-1 (ETS1).	[9]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Protein C-ets-1 (ETS1).	[10]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide decreases the expression of Protein C-ets-1 (ETS1).	[11]
Vorinostat	DMWMPD4	Approved	Vorinostat increases the expression of Protein C-ets-1 (ETS1).	[12]
Decitabine	DMQL8XJ	Approved	Decitabine increases the expression of Protein C-ets-1 (ETS1).	[13]
Zoledronate	DMIXC7G	Approved	Zoledronate increases the expression of Protein C-ets-1 (ETS1).	[14]
Fluorouracil	DMUM7HZ	Approved	Fluorouracil increases the expression of Protein C-ets-1 (ETS1).	[15]
Panobinostat	DM58WKG	Approved	Panobinostat increases the expression of Protein C-ets-1 (ETS1).	[12]
Etoposide	DMNH3PG	Approved	Etoposide increases the expression of Protein C-ets-1 (ETS1).	[15]
Sulindac	DM2QHZU	Approved	Sulindac increases the expression of Protein C-ets-1 (ETS1).	[16]
Acocantherin	DM7JT24	Approved	Acocantherin decreases the expression of Protein C-ets-1 (ETS1).	[17]
Belinostat	DM6OC53	Phase 2	Belinostat increases the expression of Protein C-ets-1 (ETS1).	[12]
ACYLINE	DM9GRTK	Phase 2	ACYLINE increases the expression of Protein C-ets-1 (ETS1).	[18]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Protein C-ets-1 (ETS1).	[19]
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Protein C-ets-1 (ETS1).	[20]
Geldanamycin	DMS7TC5	Discontinued in Phase 2	Geldanamycin increases the expression of Protein C-ets-1 (ETS1).	[22]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A increases the expression of Protein C-ets-1 (ETS1).	[24]
Milchsaure	DM462BT	Investigative	Milchsaure increases the expression of Protein C-ets-1 (ETS1).	[25]
Deguelin	DMXT7WG	Investigative	Deguelin increases the expression of Protein C-ets-1 (ETS1).	[26]
4-hydroxy-2-nonenal	DM2LJFZ	Investigative	4-hydroxy-2-nonenal decreases the expression of Protein C-ets-1 (ETS1).	[27]
Rutin	DMEHRAJ	Investigative	Rutin increases the expression of Protein C-ets-1 (ETS1).	[28]

References

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