Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTRLJK4Z)

• DOT Name: Histone H1.0 (H1-0)
• Synonyms: Histone H1'; Histone H1(0)
• Gene Name: H1-0
• Related Disease:
  Acute myelogenous leukaemia
  Advanced cancer
  Ataxia-telangiectasia
  Bladder cancer
  Cutaneous leishmaniasis
  Depression
  Hepatocellular carcinoma
  Lupus
  Mental disorder
  Systemic lupus erythematosus
  Ulcerative colitis
  Urinary bladder cancer
  Urinary bladder neoplasm
  Xeroderma pigmentosum group A
  Inclusion body myositis
  Neoplasm
  Breast cancer
  Breast carcinoma
  Prostate cancer
  Prostate carcinoma
  Small lymphocytic lymphoma
• UniProt ID: H10_HUMAN
• PDB ID: 6HQ1; 6LA2; 6LA8; 6LA9; 6LAB; 6N88; 6N89; 7COW; 7DBP; 7K5X; 7XVL; 7XX6
• Pfam ID: PF00538
• Sequence:
  MTENSTSAPAAKPKRAKASKKSTDHPKYSDMIVAAIQAEKNRAGSSRQSIQKYIKSHYKV
  GENADSQIKLSIKRLVTTGVLKQTKGVGASGSFRLAKSDEPKKSVAFKKTKKEIKKVATP
  KKASKPKKAASKAPTKKPKATPVKKAKKKLAATPKKAKKPKTVKAKPVKASKPKKAKPVK
  PKAKSSAKRAGKKK
• Function: Histones H1 are necessary for the condensation of nucleosome chains into higher-order structures. The histones H1.0 are found in cells that are in terminal stages of differentiation or that have low rates of cell division.
• Reactome Pathway:
  Formation of Senescence-Associated Heterochromatin Foci (SAHF) (R-HSA-2559584)
  Apoptosis induced DNA fragmentation (R-HSA-140342)

Molecular Interaction Atlas (MIA) of This DOT

21 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Acute myelogenous leukaemia	DISCSPTN	Strong	Biomarker	[1]
Advanced cancer	DISAT1Z9	Strong	Biomarker	[2]
Ataxia-telangiectasia	DISP3EVR	Strong	Biomarker	[3]
Bladder cancer	DISUHNM0	Strong	Posttranslational Modification	[4]
Cutaneous leishmaniasis	DISRK7TS	Strong	Biomarker	[5]
Depression	DIS3XJ69	Strong	Biomarker	[6]
Hepatocellular carcinoma	DIS0J828	Strong	Biomarker	[7]
Lupus	DISOKJWA	Strong	Biomarker	[8]
Mental disorder	DIS3J5R8	Strong	Biomarker	[6]
Systemic lupus erythematosus	DISI1SZ7	Strong	Biomarker	[9]
Ulcerative colitis	DIS8K27O	Strong	Biomarker	[10]
Urinary bladder cancer	DISDV4T7	Strong	Posttranslational Modification	[4]
Urinary bladder neoplasm	DIS7HACE	Strong	Posttranslational Modification	[4]
Xeroderma pigmentosum group A	DIS38HWC	Strong	Genetic Variation	[11]
Inclusion body myositis	DISZXXG5	moderate	Biomarker	[12]
Neoplasm	DISZKGEW	Disputed	Biomarker	[13]
Breast cancer	DIS7DPX1	Limited	Biomarker	[14]
Breast carcinoma	DIS2UE88	Limited	Biomarker	[14]
Prostate cancer	DISF190Y	Limited	Biomarker	[15]
Prostate carcinoma	DISMJPLE	Limited	Biomarker	[15]
Small lymphocytic lymphoma	DIS30POX	Limited	Altered Expression	[16]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the expression of Histone H1.0 (H1-0).	[17]
Ciclosporin	DMAZJFX	Approved	Ciclosporin increases the expression of Histone H1.0 (H1-0).	[18]
Tretinoin	DM49DUI	Approved	Tretinoin increases the expression of Histone H1.0 (H1-0).	[19]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Histone H1.0 (H1-0).	[20]
Doxorubicin	DMVP5YE	Approved	Doxorubicin increases the expression of Histone H1.0 (H1-0).	[21]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate affects the expression of Histone H1.0 (H1-0).	[22]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Histone H1.0 (H1-0).	[23]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide affects the expression of Histone H1.0 (H1-0).	[24]
Carbamazepine	DMZOLBI	Approved	Carbamazepine affects the expression of Histone H1.0 (H1-0).	[25]
Ethanol	DMDRQZU	Approved	Ethanol decreases the expression of Histone H1.0 (H1-0).	[26]
Azacitidine	DMTA5OE	Approved	Azacitidine increases the expression of Histone H1.0 (H1-0).	[27]
Urethane	DM7NSI0	Phase 4	Urethane decreases the expression of Histone H1.0 (H1-0).	[28]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Histone H1.0 (H1-0).	[29]
Belinostat	DM6OC53	Phase 2	Belinostat increases the expression of Histone H1.0 (H1-0).	[30]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Histone H1.0 (H1-0).	[31]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 increases the expression of Histone H1.0 (H1-0).	[32]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 increases the expression of Histone H1.0 (H1-0).	[33]
UNC0379	DMD1E4J	Preclinical	UNC0379 increases the expression of Histone H1.0 (H1-0).	[34]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the expression of Histone H1.0 (H1-0).	[35]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A increases the expression of Histone H1.0 (H1-0).	[30]
Sulforaphane	DMQY3L0	Investigative	Sulforaphane decreases the expression of Histone H1.0 (H1-0).	[36]
Deguelin	DMXT7WG	Investigative	Deguelin increases the expression of Histone H1.0 (H1-0).	[37]

References

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