Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT8K1UV2)

• DOT Name: Choline/ethanolaminephosphotransferase 1 (CEPT1)
• Synonyms: hCEPT1; EC 2.7.8.1; EC 2.7.8.2; 1-alkenyl-2-acylglycerol choline phosphotransferase; EC 2.7.8.22
• Gene Name: CEPT1
• UniProt ID: CEPT1_HUMAN
• PDB ID: 8GYW; 8GYX
• EC Number: 2.7.8.1; 2.7.8.2; 2.7.8.22
• Pfam ID: PF01066
• Sequence:
  MSGHRSTRKRCGDSHPESPVGFGHMSTTGCVLNKLFQLPTPPLSRHQLKRLEEHRYQSAG
  RSLLEPLMQGYWEWLVRRVPSWIAPNLITIIGLSINICTTILLVFYCPTATEQAPLWAYI
  ACACGLFIYQSLDAIDGKQARRTNSSSPLGELFDHGCDSLSTVFVVLGTCIAVQLGTNPD
  WMFFCCFAGTFMFYCAHWQTYVSGTLRFGIIDVTEVQIFIIIMHLLAVIGGPPFWQSMIP
  VLNIQMKIFPALCTVAGTIFSCTNYFRVIFTGGVGKNGSTIAGTSVLSPFLHIGSVITLA
  AMIYKKSAVQLFEKHPCLYILTFGFVSAKITNKLVVAHMTKSEMHLHDTAFIGPALLFLD
  QYFNSFIDEYIVLWIALVFSFFDLIRYCVSVCNQIASHLHIHVFRIKVSTAHSNHH
• Function: Catalyzes both phosphatidylcholine and phosphatidylethanolamine biosynthesis from CDP-choline and CDP-ethanolamine, respectively. Involved in protein-dependent process of phospholipid transport to distribute phosphatidyl choline to the lumenal surface. Has a higher cholinephosphotransferase activity than ethanolaminephosphotransferase activity.
• Tissue Specificity: Ubiquitously expressed.
• KEGG Pathway:
  Phospho.te and phosphi.te metabolism (hsa00440)
  Glycerophospholipid metabolism (hsa00564)
  Ether lipid metabolism (hsa00565)
  Metabolic pathways (hsa01100)
• Reactome Pathway:
  Synthesis of PE (R-HSA-1483213)
  Synthesis of PC (R-HSA-1483191)
• BioCyc Pathway: MetaCyc:HS05844-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

8 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 Choline/ethanolaminephosphotransferase 1 (CEPT1).	[1]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[2]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[3]
Carbamazepine	DMZOLBI	Approved	Carbamazepine affects the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[4]
Zoledronate	DMIXC7G	Approved	Zoledronate increases the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[5]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 increases the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[7]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[8]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A increases the expression of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[9]

1 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 decreases the sumoylation of Choline/ethanolaminephosphotransferase 1 (CEPT1).	[6]

References

• [1] Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
• [2] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [3] The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
• [4] Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
• [5] Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
• [6] Inhibiting ubiquitination causes an accumulation of SUMOylated newly synthesized nuclear proteins at PML bodies. J Biol Chem. 2019 Oct 18;294(42):15218-15234. doi: 10.1074/jbc.RA119.009147. Epub 2019 Jul 8.
• [7] Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.
• [8] Alternatives for the worse: Molecular insights into adverse effects of bisphenol a and substitutes during human adipocyte differentiation. Environ Int. 2021 Nov;156:106730. doi: 10.1016/j.envint.2021.106730. Epub 2021 Jun 27.
• [9] From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.