Details of Drug Off-Target (DOT)

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

• DOT Name: N-acetyltransferase ESCO2 (ESCO2)
• Synonyms: EC 2.3.1.-; Establishment factor-like protein 2; EFO2; EFO2p; hEFO2; Establishment of cohesion 1 homolog 2; ECO1 homolog 2
• Gene Name: ESCO2
• Related Disease:
  Roberts-SC phocomelia syndrome
  Advanced cancer
  Colorectal carcinoma
  Cornelia de Lange syndrome
  Kidney cancer
  Kidney neoplasm
  Metastatic malignant neoplasm
  Obsolete Roberts syndrome
  Periodontal disease
  Influenza
  Leukemia
  Autism spectrum disorder
  Gastric cancer
  Neoplasm
  Stomach cancer
• UniProt ID: ESCO2_HUMAN
• EC Number: 2.3.1.-
• Pfam ID: PF13880 ; PF13878
• Sequence:
  MAALTPRKRKQDSLKCDSLLHFTENLFPSPNKKHCFYQNSDKNEENLHCSQQEHFVLSAL
  KTTEINRLPSANQGSPFKSALSTVSFYNQNKWYLNPLERKLIKESRSTCLKTNDEDKSFP
  IVTEKMQGKPVCSKKNNKKPQKSLTAKYQPKYRHIKPVSRNSRNSKQNRVIYKPIVEKEN
  NCHSAENNSNAPRVLSQKIKPQVTLQGGAAFFVRKKSSLRKSSLENEPSLGRTQKSKSEV
  IEDSDVETVSEKKTFATRQVPKCLVLEEKLKIGLLSASSKNKEKLIKDSSDDRVSSKEHK
  VDKNEAFSSEDSLGENKTISPKSTVYPIFSASSVNSKRSLGEEQFSVGSVNFMKQTNIQK
  NTNTRDTSKKTKDQLIIDAGQKHFGATVCKSCGMIYTASNPEDEMQHVQHHHRFLEGIKY
  VGWKKERVVAEFWDGKIVLVLPHDPSFAIKKVEDVQELVDNELGFQQVVPKCPNKIKTFL
  FISDEKRVVGCLIAEPIKQAFRVLSEPIGPESPSSTECPRAWQCSDVPEPAVCGISRIWV
  FRLKRRKRIARRLVDTLRNCFMFGCFLSTDEIAFSDPTPDGKLFATKYCNTPNFLVYNFN
  S
• Function: Acetyltransferase required for the establishment of sister chromatid cohesion. Couples the processes of cohesion and DNA replication to ensure that only sister chromatids become paired together. In contrast to the structural cohesins, the deposition and establishment factors are required only during the S phase. Acetylates the cohesin component SMC3.
• Tissue Specificity: Widely expressed in fetal tissues. In adult, it is expressed in thymus, placenta and small intestine.
• KEGG Pathway: Cell cycle (hsa04110)
• Reactome Pathway: Establishment of Sister Chromatid Cohesion (R-HSA-2468052)

Molecular Interaction Atlas (MIA) of This DOT

15 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Roberts-SC phocomelia syndrome	DIS4JXZ4	Definitive	Autosomal recessive	[1]
Advanced cancer	DISAT1Z9	Strong	Biomarker	[2]
Colorectal carcinoma	DIS5PYL0	Strong	Altered Expression	[3]
Cornelia de Lange syndrome	DISEQSXO	Strong	Biomarker	[4]
Kidney cancer	DISBIPKM	Strong	Biomarker	[5]
Kidney neoplasm	DISBNZTN	Strong	Biomarker	[5]
Metastatic malignant neoplasm	DIS86UK6	Strong	Biomarker	[3]
Obsolete Roberts syndrome	DISLY197	Strong	Autosomal recessive	[6]
Periodontal disease	DISJQHVN	Strong	Altered Expression	[7]
Influenza	DIS3PNU3	moderate	Altered Expression	[8]
Leukemia	DISNAKFL	moderate	Biomarker	[9]
Autism spectrum disorder	DISXK8NV	Limited	Biomarker	[10]
Gastric cancer	DISXGOUK	Limited	Biomarker	[11]
Neoplasm	DISZKGEW	Limited	Biomarker	[11]
Stomach cancer	DISKIJSX	Limited	Biomarker	[11]

21 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 N-acetyltransferase ESCO2 (ESCO2).	[12]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[13]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[14]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[15]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[16]
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of N-acetyltransferase ESCO2 (ESCO2).	[17]
Calcitriol	DM8ZVJ7	Approved	Calcitriol decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[18]
Vorinostat	DMWMPD4	Approved	Vorinostat affects the expression of N-acetyltransferase ESCO2 (ESCO2).	[19]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[18]
Zoledronate	DMIXC7G	Approved	Zoledronate increases the expression of N-acetyltransferase ESCO2 (ESCO2).	[20]
Demecolcine	DMCZQGK	Approved	Demecolcine decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[21]
Azathioprine	DMMZSXQ	Approved	Azathioprine decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[22]
Lucanthone	DMZLBUO	Approved	Lucanthone decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[23]
Urethane	DM7NSI0	Phase 4	Urethane decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[24]
GSK2110183	DMZHB37	Phase 2	GSK2110183 decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[25]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[26]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[28]
Geldanamycin	DMS7TC5	Discontinued in Phase 2	Geldanamycin increases the expression of N-acetyltransferase ESCO2 (ESCO2).	[30]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[31]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of N-acetyltransferase ESCO2 (ESCO2).	[32]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of N-acetyltransferase ESCO2 (ESCO2).	[33]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
TAK-243	DM4GKV2	Phase 1	TAK-243 increases the sumoylation of N-acetyltransferase ESCO2 (ESCO2).	[27]
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 decreases the phosphorylation of N-acetyltransferase ESCO2 (ESCO2).	[29]
Coumarin	DM0N8ZM	Investigative	Coumarin increases the phosphorylation of N-acetyltransferase ESCO2 (ESCO2).	[29]

References

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