Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTQRUIJ4)

DOT Name Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT)
Synonyms CS-KMT; EC 2.1.1.-; Methyltransferase-like protein 12, mitochondrial
Gene Name CSKMT
UniProt ID
CSKMT_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
2.1.1.-
Pfam ID
PF13847
Sequence
MAALRRMLHLPSLMMGTCRPFAGSLADSCLADRCLWDRLHAQPRLGTVPTFDWFFGYDEV
QGLLLPLLQEAQAASPLRVLDVGCGTSSLCTGLYTKSPHPVDVLGVDFSPVAVAHMNSLL
EGGPGQTPLCPGHPASSLHFMHADAQNLGAVASSGSFQLLLDKGTWDAVARGGLPRAYQL
LSECLRVLNPQGTLIQFSDEDPDVRLPCLEQGSYGWTVTVQELGPFRGITYFAYLIQGSH
Function
Protein-lysine methyltransferase that selectively trimethylates citrate synthase (CS) in mitochondria. Seems to conduct trimethylation in a highly distributive manner rather than in a processive manner, and thus introduces a single methyl group per binding event.

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
7 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [1]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [2]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [3]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [4]
Quercetin DM3NC4M Approved Quercetin increases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [5]
Testosterone DM7HUNW Approved Testosterone decreases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [6]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 increases the expression of Citrate synthase-lysine N-methyltransferase CSKMT, mitochondrial (CSKMT). [7]
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References

1 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
2 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
3 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
4 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
5 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.
6 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.
7 Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma. Oncotarget. 2014 May 15;5(9):2355-71.