Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTVVV668)

• DOT Name: Lymphoid-specific helicase (HELLS)
• Synonyms: EC 3.6.4.-; Proliferation-associated SNF2-like protein; SWI/SNF2-related matrix-associated actin-dependent regulator of chromatin subfamily A member 6
• Gene Name: HELLS
• Related Disease:
  Adult glioblastoma
  Astrocytoma
  Autoimmune disease
  B-cell lymphoma
  B-cell neoplasm
  Breast cancer
  Breast carcinoma
  Burkitt lymphoma
  Colorectal carcinoma
  Epstein barr virus infection
  Gastric cancer
  Glioblastoma multiforme
  Glioma
  Head-neck squamous cell carcinoma
  Immunodeficiency-centromeric instability-facial anomalies syndrome 4
  Medulloblastoma
  Mycosis fungoides
  Neoplasm
  Oropharyngeal squamous cell carcinoma
  Polycystic ovarian syndrome
  Retinoblastoma
  Sezary syndrome
  Stomach cancer
  Hepatocellular carcinoma
  Immunodeficiency-centromeric instability-facial anomalies syndrome
  Lung adenocarcinoma
  Prostate cancer
  Prostate carcinoma
  Advanced cancer
  Bone osteosarcoma
  Clear cell renal carcinoma
  Lung cancer
  Lung carcinoma
  Non-small-cell lung cancer
  Osteosarcoma
• UniProt ID: HELLS_HUMAN
• EC Number: 3.6.4.-
• Pfam ID: PF00271 ; PF00176
• Sequence:
  MPAERPAGSGGSEAPAMVEQLDTAVITPAMLEEEEQLEAAGLERERKMLEKARMSWDRES
  TEIRYRRLQHLLEKSNIYSKFLLTKMEQQQLEEQKKKEKLERKKESLKVKKGKNSIDASE
  EKPVMRKKRGREDESYNISEVMSKEEILSVAKKNKKENEDENSSSTNLCVEDLQKNKDSN
  SIIKDRLSETVRQNTKFFFDPVRKCNGQPVPFQQPKHFTGGVMRWYQVEGMEWLRMLWEN
  GINGILADEMGLGKTVQCIATIALMIQRGVPGPFLVCGPLSTLPNWMAEFKRFTPDIPTM
  LYHGTQEERQKLVRNIYKRKGTLQIHPVVITSFEIAMRDRNALQHCYWKYLIVDEGHRIK
  NMKCRLIRELKRFNADNKLLLTGTPLQNNLSELWSLLNFLLPDVFDDLKSFESWFDITSL
  SETAEDIIAKEREQNVLHMLHQILTPFLLRRLKSDVALEVPPKREVVVYAPLSKKQEIFY
  TAIVNRTIANMFGSSEKETIELSPTGRPKRRTRKSINYSKIDDFPNELEKLISQIQPEVD
  RERAVVEVNIPVESEVNLKLQNIMMLLRKCCNHPYLIEYPIDPVTQEFKIDEELVTNSGK
  FLILDRMLPELKKRGHKVLLFSQMTSMLDILMDYCHLRDFNFSRLDGSMSYSEREKNMHS
  FNTDPEVFIFLVSTRAGGLGINLTAADTVIIYDSDWNPQSDLQAQDRCHRIGQTKPVVVY
  RLVTANTIDQKIVERAAAKRKLEKLIIHKNHFKGGQSGLNLSKNFLDPKELMELLKSRDY
  EREIKGSREKVISDKDLELLLDRSDLIDQMNASGPIKEKMGIFKILENSEDSSPECLF
• Function: Plays an essential role in normal development and survival. Involved in regulation of the expansion or survival of lymphoid cells. Required for de novo or maintenance DNA methylation. May control silencing of the imprinted CDKN1C gene through DNA methylation. May play a role in formation and organization of heterochromatin, implying a functional role in the regulation of transcription and mitosis.
• Tissue Specificity: Highly expressed in proliferative tissues such as adult thymus and testis, and expressed at lower levels in uterus, small intestine, colon, and peripheral blood mononuclear cells. Also expressed in neoplastic cell lines including those derived from myeloid and lymphoid leukemias.

Molecular Interaction Atlas (MIA) of This DOT

35 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Adult glioblastoma	DISVP4LU	Strong	Biomarker	[1]
Astrocytoma	DISL3V18	Strong	Altered Expression	[2]
Autoimmune disease	DISORMTM	Strong	Biomarker	[3]
B-cell lymphoma	DISIH1YQ	Strong	Biomarker	[4]
B-cell neoplasm	DISVY326	Strong	Biomarker	[4]
Breast cancer	DIS7DPX1	Strong	Biomarker	[5]
Breast carcinoma	DIS2UE88	Strong	Biomarker	[5]
Burkitt lymphoma	DIS9D5XU	Strong	Biomarker	[4]
Colorectal carcinoma	DIS5PYL0	Strong	Biomarker	[6]
Epstein barr virus infection	DISOO0WT	Strong	Biomarker	[4]
Gastric cancer	DISXGOUK	Strong	Genetic Variation	[7]
Glioblastoma multiforme	DISK8246	Strong	Biomarker	[1]
Glioma	DIS5RPEH	Strong	Altered Expression	[1]
Head-neck squamous cell carcinoma	DISF7P24	Strong	Altered Expression	[8]
Immunodeficiency-centromeric instability-facial anomalies syndrome 4	DISM0EDE	Strong	Autosomal recessive	[9]
Medulloblastoma	DISZD2ZL	Strong	Biomarker	[10]
Mycosis fungoides	DIS62RB8	Strong	Biomarker	[11]
Neoplasm	DISZKGEW	Strong	Altered Expression	[1]
Oropharyngeal squamous cell carcinoma	DIS7D7QV	Strong	Altered Expression	[12]
Polycystic ovarian syndrome	DISZ2BNG	Strong	Biomarker	[13]
Retinoblastoma	DISVPNPB	Strong	Biomarker	[14]
Sezary syndrome	DISFMTC7	Strong	Biomarker	[11]
Stomach cancer	DISKIJSX	Strong	Genetic Variation	[7]
Hepatocellular carcinoma	DIS0J828	moderate	Biomarker	[15]
Immunodeficiency-centromeric instability-facial anomalies syndrome	DISQ0KIE	Supportive	Autosomal recessive	[9]
Lung adenocarcinoma	DISD51WR	Disputed	Biomarker	[16]
Prostate cancer	DISF190Y	Disputed	Altered Expression	[17]
Prostate carcinoma	DISMJPLE	Disputed	Altered Expression	[17]
Advanced cancer	DISAT1Z9	Limited	Biomarker	[18]
Bone osteosarcoma	DIST1004	Limited	Biomarker	[19]
Clear cell renal carcinoma	DISBXRFJ	Limited	Altered Expression	[20]
Lung cancer	DISCM4YA	Limited	Biomarker	[21]
Lung carcinoma	DISTR26C	Limited	Biomarker	[21]
Non-small-cell lung cancer	DIS5Y6R9	Limited	Biomarker	[21]
Osteosarcoma	DISLQ7E2	Limited	Biomarker	[19]

29 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 Lymphoid-specific helicase (HELLS).	[22]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Lymphoid-specific helicase (HELLS).	[23]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Lymphoid-specific helicase (HELLS).	[24]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Lymphoid-specific helicase (HELLS).	[25]
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of Lymphoid-specific helicase (HELLS).	[26]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of Lymphoid-specific helicase (HELLS).	[27]
Ivermectin	DMDBX5F	Approved	Ivermectin decreases the expression of Lymphoid-specific helicase (HELLS).	[28]
Quercetin	DM3NC4M	Approved	Quercetin affects the expression of Lymphoid-specific helicase (HELLS).	[29]
Calcitriol	DM8ZVJ7	Approved	Calcitriol decreases the expression of Lymphoid-specific helicase (HELLS).	[30]
Vorinostat	DMWMPD4	Approved	Vorinostat increases the expression of Lymphoid-specific helicase (HELLS).	[31]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of Lymphoid-specific helicase (HELLS).	[30]
Marinol	DM70IK5	Approved	Marinol increases the expression of Lymphoid-specific helicase (HELLS).	[32]
Progesterone	DMUY35B	Approved	Progesterone decreases the expression of Lymphoid-specific helicase (HELLS).	[33]
Demecolcine	DMCZQGK	Approved	Demecolcine decreases the expression of Lymphoid-specific helicase (HELLS).	[34]
Diethylstilbestrol	DMN3UXQ	Approved	Diethylstilbestrol decreases the expression of Lymphoid-specific helicase (HELLS).	[35]
Azathioprine	DMMZSXQ	Approved	Azathioprine decreases the expression of Lymphoid-specific helicase (HELLS).	[36]
Irinotecan	DMP6SC2	Approved	Irinotecan decreases the expression of Lymphoid-specific helicase (HELLS).	[37]
Dasatinib	DMJV2EK	Approved	Dasatinib decreases the expression of Lymphoid-specific helicase (HELLS).	[38]
Urethane	DM7NSI0	Phase 4	Urethane decreases the expression of Lymphoid-specific helicase (HELLS).	[39]
Resveratrol	DM3RWXL	Phase 3	Resveratrol decreases the expression of Lymphoid-specific helicase (HELLS).	[40]
GSK2110183	DMZHB37	Phase 2	GSK2110183 decreases the expression of Lymphoid-specific helicase (HELLS).	[41]
PEITC	DMOMN31	Phase 2	PEITC decreases the expression of Lymphoid-specific helicase (HELLS).	[42]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Lymphoid-specific helicase (HELLS).	[43]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 increases the expression of Lymphoid-specific helicase (HELLS).	[44]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Lymphoid-specific helicase (HELLS).	[46]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Lymphoid-specific helicase (HELLS).	[48]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of Lymphoid-specific helicase (HELLS).	[34]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of Lymphoid-specific helicase (HELLS).	[27]
Deguelin	DMXT7WG	Investigative	Deguelin increases the expression of Lymphoid-specific helicase (HELLS).	[49]

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 Lymphoid-specific helicase (HELLS).	[45]
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 increases the phosphorylation of Lymphoid-specific helicase (HELLS).	[47]
Coumarin	DM0N8ZM	Investigative	Coumarin increases the phosphorylation of Lymphoid-specific helicase (HELLS).	[47]

References

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