Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTN9P0BO)

• DOT Name: Histone H2A type 1 (H2AC11)
• Synonyms: H2A.1; Histone H2A/ptl
• Gene Name: H2AC11
• Related Disease:
  Advanced cancer
  Epithelial ovarian cancer
  Major depressive disorder
  Ovarian cancer
  Ovarian neoplasm
• UniProt ID: H2A1_HUMAN
• PDB ID: 4QYL; 5KGF; 6R0C; 6RNY; 6X59; 6X5A; 6XJD; 7BG9; 7E8D; 7JO9; 7JOA; 7TAN; 7U50; 7U51; 7U52; 7U53; 7UV9; 8ATF; 8AV6; 8GUI; 8GUJ; 8GUK; 8OFF
• Pfam ID: PF00125 ; PF16211
• Sequence:
  MSGRGKQGGKARAKAKTRSSRAGLQFPVGRVHRLLRKGNYAERVGAGAPVYLAAVLEYLT
  AEILELAGNAARDNKKTRIIPRHLQLAIRNDEELNKLLGKVTIAQGGVLPNIQAVLLPKK
  TESHHKAKGK
• Function: Core component of nucleosome. Nucleosomes wrap and compact DNA into chromatin, limiting DNA accessibility to the cellular machineries which require DNA as a template. Histones thereby play a central role in transcription regulation, DNA repair, DNA replication and chromosomal stability. DNA accessibility is regulated via a complex set of post-translational modifications of histones, also called histone code, and nucleosome remodeling.
• KEGG Pathway:
  ATP-dependent chromatin remodeling (hsa03082)
  Necroptosis (hsa04217)
  Neutrophil extracellular trap formation (hsa04613)
  Alcoholism (hsa05034)
  Systemic lupus erythematosus (hsa05322)
• Reactome Pathway:
  HATs acetylate histones (R-HSA-3214847)
  RMTs methylate histone arginines (R-HSA-3214858)
  UCH proteinases (R-HSA-5689603)
  Ub-specific processing proteases (R-HSA-5689880)
  Metalloprotease DUBs (R-HSA-5689901)
  HCMV Early Events (R-HSA-9609690)
  HCMV Late Events (R-HSA-9610379)
  HDACs deacetylate histones (R-HSA-3214815)

Molecular Interaction Atlas (MIA) of This DOT

5 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Advanced cancer	DISAT1Z9	Strong	Biomarker	[1]
Epithelial ovarian cancer	DIS56MH2	Strong	Biomarker	[1]
Major depressive disorder	DIS4CL3X	Strong	Biomarker	[2]
Ovarian cancer	DISZJHAP	Strong	Biomarker	[1]
Ovarian neoplasm	DISEAFTY	Strong	Biomarker	[1]

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 Histone H2A type 1 (H2AC11).	[3]
Arsenic	DMTL2Y1	Approved	Arsenic affects the methylation of Histone H2A type 1 (H2AC11).	[9]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the methylation of Histone H2A type 1 (H2AC11).	[22]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Histone H2A type 1 (H2AC11).	[4]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Histone H2A type 1 (H2AC11).	[5]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Histone H2A type 1 (H2AC11).	[6]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of Histone H2A type 1 (H2AC11).	[7]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Histone H2A type 1 (H2AC11).	[8]
Calcitriol	DM8ZVJ7	Approved	Calcitriol decreases the expression of Histone H2A type 1 (H2AC11).	[10]
Testosterone	DM7HUNW	Approved	Testosterone increases the expression of Histone H2A type 1 (H2AC11).	[10]
Demecolcine	DMCZQGK	Approved	Demecolcine increases the expression of Histone H2A type 1 (H2AC11).	[11]
Cannabidiol	DM0659E	Approved	Cannabidiol decreases the expression of Histone H2A type 1 (H2AC11).	[12]
Isotretinoin	DM4QTBN	Approved	Isotretinoin decreases the expression of Histone H2A type 1 (H2AC11).	[13]
Hydroquinone	DM6AVR4	Approved	Hydroquinone decreases the expression of Histone H2A type 1 (H2AC11).	[14]
Lucanthone	DMZLBUO	Approved	Lucanthone decreases the expression of Histone H2A type 1 (H2AC11).	[15]
Liothyronine	DM6IR3P	Approved	Liothyronine decreases the expression of Histone H2A type 1 (H2AC11).	[16]
Berberine	DMC5Q8X	Phase 4	Berberine decreases the expression of Histone H2A type 1 (H2AC11).	[17]
Genistein	DM0JETC	Phase 2/3	Genistein decreases the expression of Histone H2A type 1 (H2AC11).	[18]
Amiodarone	DMUTEX3	Phase 2/3 Trial	Amiodarone increases the expression of Histone H2A type 1 (H2AC11).	[19]
GSK2110183	DMZHB37	Phase 2	GSK2110183 decreases the expression of Histone H2A type 1 (H2AC11).	[20]
PEITC	DMOMN31	Phase 2	PEITC decreases the expression of Histone H2A type 1 (H2AC11).	[21]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Histone H2A type 1 (H2AC11).	[23]
PMID28870136-Compound-48	DMPIM9L	Patented	PMID28870136-Compound-48 decreases the expression of Histone H2A type 1 (H2AC11).	[24]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Histone H2A type 1 (H2AC11).	[25]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of Histone H2A type 1 (H2AC11).	[11]
Milchsaure	DM462BT	Investigative	Milchsaure increases the expression of Histone H2A type 1 (H2AC11).	[26]
Coumestrol	DM40TBU	Investigative	Coumestrol decreases the expression of Histone H2A type 1 (H2AC11).	[8]
Deguelin	DMXT7WG	Investigative	Deguelin increases the expression of Histone H2A type 1 (H2AC11).	[27]
methyl p-hydroxybenzoate	DMO58UW	Investigative	methyl p-hydroxybenzoate decreases the expression of Histone H2A type 1 (H2AC11).	[28]
Lithium chloride	DMHYLQ2	Investigative	Lithium chloride decreases the expression of Histone H2A type 1 (H2AC11).	[29]

References

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