Details of Drug Off-Target (DOT)

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

• DOT Name: EEF1A lysine methyltransferase 1 (EEF1AKMT1)
• Synonyms: EC 2.1.1.-; N(6)-adenine-specific DNA methyltransferase 2; Protein-lysine N-methyltransferase N6AMT2; eEF1A-KMT
• Gene Name: EEF1AKMT1
• UniProt ID: EFMT1_HUMAN
• EC Number: 2.1.1.-
• Pfam ID: PF10237
• Sequence:
  MSDLEDDETPQLSAHALAALQEFYAEQKQQIEPGEDDKYNIGIIEENWQLSQFWYSQETA
  LQLAQEAIAAVGEGGRIACVSAPSVYQKLRELCRENFSIYIFEYDKRFAMYGEEFIFYDY
  NNPLDLPERIAAHSFDIVIADPPYLSEECLRKTSETVKYLTRGKILLCTGAIMEEQAAEL
  LGVKMCTFVPRHTRNLANEFRCYVNYDSGLDCGI
• Function: Protein N-lysine methyltransferase that selectively catalyzes the trimethylation of EEF1A at 'Lys-79'.
• Reactome Pathway: Protein methylation (R-HSA-8876725)

Molecular Interaction Atlas (MIA) of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of EEF1A lysine methyltransferase 1 (EEF1AKMT1).	[1]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of EEF1A lysine methyltransferase 1 (EEF1AKMT1).	[2]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of EEF1A lysine methyltransferase 1 (EEF1AKMT1).	[3]
Temozolomide	DMKECZD	Approved	Temozolomide increases the expression of EEF1A lysine methyltransferase 1 (EEF1AKMT1).	[4]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of EEF1A lysine methyltransferase 1 (EEF1AKMT1).	[5]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 increases the phosphorylation of EEF1A lysine methyltransferase 1 (EEF1AKMT1).	[6]

References

• [1] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [2] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [3] Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
• [4] Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
• [5] 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.
• [6] Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.