Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT8VYY84)

• DOT Name: Chromobox protein homolog 5 (CBX5)
• Synonyms: Antigen p25; Heterochromatin protein 1 homolog alpha; HP1 alpha
• Gene Name: CBX5
• Related Disease:
  Colorectal carcinoma
  Colorectal neoplasm
  Adenocarcinoma
  Adult teratoma
  Alzheimer disease
  Brain neoplasm
  Breast cancer
  Breast carcinoma
  Breast neoplasm
  Carcinoma
  Carcinoma of liver and intrahepatic biliary tract
  Cerebral infarction
  Cholangiocarcinoma
  Colon cancer
  Colon carcinoma
  Congenital contractural arachnodactyly
  Congenital dyserythropoietic anemia type 1
  Glioma
  Liver cancer
  Lung cancer
  Lung carcinoma
  Major depressive disorder
  Neoplasm
  Nijmegen breakage syndrome
  Non-small-cell lung cancer
  Prostate cancer
  Prostate carcinoma
  Pulmonary fibrosis
  Seminoma
  Systemic sclerosis
  Teratoma
  Thyroid gland carcinoma
  Malaria
  Bladder cancer
  Gastric cancer
  Stomach cancer
  Urinary bladder cancer
  Urinary bladder neoplasm
• UniProt ID: CBX5_HUMAN
• PDB ID: 3FDT; 3I3C
• Pfam ID: PF00385 ; PF01393
• Sequence:
  MGKKTKRTADSSSSEDEEEYVVEKVLDRRVVKGQVEYLLKWKGFSEEHNTWEPEKNLDCP
  ELISEFMKKYKKMKEGENNKPREKSESNKRKSNFSNSADDIKSKKKREQSNDIARGFERG
  LEPEKIIGATDSCGDLMFLMKWKDTDEADLVLAKEANVKCPQIVIAFYEERLTWHAYPED
  AENKEKETAKS
• Function: Component of heterochromatin that recognizes and binds histone H3 tails methylated at 'Lys-9' (H3K9me), leading to epigenetic repression. In contrast, it is excluded from chromatin when 'Tyr-41' of histone H3 is phosphorylated (H3Y41ph). Can interact with lamin-B receptor (LBR). This interaction can contribute to the association of the heterochromatin with the inner nuclear membrane. Involved in the formation of functional kinetochore through interaction with MIS12 complex proteins.
• Reactome Pathway:
  Transcriptional Regulation by E2F6 (R-HSA-8953750)
  Factors involved in megakaryocyte development and platelet production (R-HSA-983231)
  SUMOylation of chromatin organization proteins (R-HSA-4551638)

Molecular Interaction Atlas (MIA) of This DOT

38 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Colorectal carcinoma	DIS5PYL0	Definitive	Biomarker	[1]
Colorectal neoplasm	DISR1UCN	Definitive	Biomarker	[1]
Adenocarcinoma	DIS3IHTY	Strong	Genetic Variation	[2]
Adult teratoma	DISBY81U	Strong	Biomarker	[3]
Alzheimer disease	DISF8S70	Strong	Genetic Variation	[4]
Brain neoplasm	DISY3EKS	Strong	Biomarker	[5]
Breast cancer	DIS7DPX1	Strong	Posttranslational Modification	[6]
Breast carcinoma	DIS2UE88	Strong	Posttranslational Modification	[6]
Breast neoplasm	DISNGJLM	Strong	Biomarker	[7]
Carcinoma	DISH9F1N	Strong	Altered Expression	[8]
Carcinoma of liver and intrahepatic biliary tract	DIS8WA0W	Strong	Genetic Variation	[9]
Cerebral infarction	DISR1WNP	Strong	Biomarker	[10]
Cholangiocarcinoma	DIS71F6X	Strong	Altered Expression	[11]
Colon cancer	DISVC52G	Strong	Biomarker	[12]
Colon carcinoma	DISJYKUO	Strong	Biomarker	[12]
Congenital contractural arachnodactyly	DISOM1K7	Strong	Biomarker	[11]
Congenital dyserythropoietic anemia type 1	DISCBVO6	Strong	Biomarker	[13]
Glioma	DIS5RPEH	Strong	Altered Expression	[5]
Liver cancer	DISDE4BI	Strong	Genetic Variation	[9]
Lung cancer	DISCM4YA	Strong	Biomarker	[14]
Lung carcinoma	DISTR26C	Strong	Biomarker	[14]
Major depressive disorder	DIS4CL3X	Strong	Biomarker	[15]
Neoplasm	DISZKGEW	Strong	Altered Expression	[2]
Nijmegen breakage syndrome	DIS98HVL	Strong	Biomarker	[16]
Non-small-cell lung cancer	DIS5Y6R9	Strong	Biomarker	[17]
Prostate cancer	DISF190Y	Strong	Altered Expression	[2]
Prostate carcinoma	DISMJPLE	Strong	Altered Expression	[2]
Pulmonary fibrosis	DISQKVLA	Strong	Biomarker	[18]
Seminoma	DIS3J8LJ	Strong	Altered Expression	[3]
Systemic sclerosis	DISF44L6	Strong	Biomarker	[19]
Teratoma	DIS6ICY4	Strong	Biomarker	[3]
Thyroid gland carcinoma	DISMNGZ0	Strong	Biomarker	[8]
Malaria	DISQ9Y50	Disputed	Altered Expression	[20]
Bladder cancer	DISUHNM0	Limited	Altered Expression	[21]
Gastric cancer	DISXGOUK	Limited	Altered Expression	[22]
Stomach cancer	DISKIJSX	Limited	Altered Expression	[22]
Urinary bladder cancer	DISDV4T7	Limited	Altered Expression	[21]
Urinary bladder neoplasm	DIS7HACE	Limited	Altered Expression	[21]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the expression of Chromobox protein homolog 5 (CBX5).	[23]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Chromobox protein homolog 5 (CBX5).	[24]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Chromobox protein homolog 5 (CBX5).	[25]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Chromobox protein homolog 5 (CBX5).	[26]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Chromobox protein homolog 5 (CBX5).	[27]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Chromobox protein homolog 5 (CBX5).	[28]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of Chromobox protein homolog 5 (CBX5).	[29]
Ivermectin	DMDBX5F	Approved	Ivermectin decreases the expression of Chromobox protein homolog 5 (CBX5).	[30]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Chromobox protein homolog 5 (CBX5).	[31]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide affects the expression of Chromobox protein homolog 5 (CBX5).	[32]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Chromobox protein homolog 5 (CBX5).	[33]
Marinol	DM70IK5	Approved	Marinol increases the expression of Chromobox protein homolog 5 (CBX5).	[34]
Zoledronate	DMIXC7G	Approved	Zoledronate increases the expression of Chromobox protein homolog 5 (CBX5).	[35]
Selenium	DM25CGV	Approved	Selenium decreases the expression of Chromobox protein homolog 5 (CBX5).	[36]
Demecolcine	DMCZQGK	Approved	Demecolcine decreases the expression of Chromobox protein homolog 5 (CBX5).	[37]
Ethanol	DMDRQZU	Approved	Ethanol decreases the expression of Chromobox protein homolog 5 (CBX5).	[38]
Testosterone enanthate	DMB6871	Approved	Testosterone enanthate affects the expression of Chromobox protein homolog 5 (CBX5).	[39]
Urethane	DM7NSI0	Phase 4	Urethane decreases the expression of Chromobox protein homolog 5 (CBX5).	[40]
SNDX-275	DMH7W9X	Phase 3	SNDX-275 decreases the expression of Chromobox protein homolog 5 (CBX5).	[33]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Chromobox protein homolog 5 (CBX5).	[41]
Tocopherol	DMBIJZ6	Phase 2	Tocopherol decreases the expression of Chromobox protein homolog 5 (CBX5).	[36]
PEITC	DMOMN31	Phase 2	PEITC decreases the expression of Chromobox protein homolog 5 (CBX5).	[42]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 increases the expression of Chromobox protein homolog 5 (CBX5).	[44]
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Chromobox protein homolog 5 (CBX5).	[45]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Chromobox protein homolog 5 (CBX5).	[47]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Chromobox protein homolog 5 (CBX5).	[48]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Chromobox protein homolog 5 (CBX5).	[49]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde decreases the expression of Chromobox protein homolog 5 (CBX5).	[37]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of Chromobox protein homolog 5 (CBX5).	[50]
methyl p-hydroxybenzoate	DMO58UW	Investigative	methyl p-hydroxybenzoate decreases the expression of Chromobox protein homolog 5 (CBX5).	[51]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Chromobox protein homolog 5 (CBX5).	[43]
TAK-243	DM4GKV2	Phase 1	TAK-243 decreases the sumoylation of Chromobox protein homolog 5 (CBX5).	[46]

References

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