General Information of Drug Off-Target (DOT) (ID: OTAG9V0I)

DOT Name General transcription factor IIE subunit 1 (GTF2E1)
Synonyms General transcription factor IIE 56 kDa subunit; Transcription initiation factor IIE subunit alpha; TFIIE-alpha
Gene Name GTF2E1
UniProt ID
T2EA_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
1VD4 ; 2JTX ; 2RNQ ; 2RNR ; 5GPY ; 5IY6 ; 5IY7 ; 5IY8 ; 5IY9 ; 5IYA ; 5IYB ; 5IYC ; 5IYD ; 6O9L ; 7EG9 ; 7EGA ; 7EGB ; 7EGC ; 7ENA ; 7ENC ; 7LBM ; 7NVR ; 7NVS ; 7NVT ; 7NVU ; 7NVV ; 7NVW ; 7NVX ; 7NVY ; 7NVZ ; 7NW0 ; 8BVW ; 8BYQ ; 8GXQ ; 8GXS ; 8WAK ; 8WAL ; 8WAN ; 8WAO ; 8WAP ; 8WAQ ; 8WAR ; 8WAS
Pfam ID
PF08271 ; PF11521 ; PF02002
Sequence
MADPDVLTEVPAALKRLAKYVIRGFYGIEHALALDILIRNSCVKEEDMLELLKFDRKQLR
SVLNNLKGDKFIKCRMRVETAADGKTTRHNYYFINYRTLVNVVKYKLDHMRRRIETDERD
STNRASFKCPVCSSTFTDLEANQLFDPMTGTFRCTFCHTEVEEDESAMPKKDARTLLARF
NEQIEPIYALLRETEDVNLAYEILEPEPTEIPALKQSKDHAATTAGAASLAGGHHREAWA
TKGPSYEDLYTQNVVINMDDQEDLHRASLEGKSAKERPIWLRESTVQGAYGSEDMKEGGI
DMDAFQEREEGHAGPDDNEEVMRALLIHEKKTSSAMAGSVGAAAPVTAANGSDSESETSE
SDDDSPPRPAAVAVHKREEDEEEDDEFEEVADDPIVMVAGRPFSYSEVSQRPELVAQMTP
EEKEAYIAMGQRMFEDLFE
Function
Recruits TFIIH to the initiation complex and stimulates the RNA polymerase II C-terminal domain kinase and DNA-dependent ATPase activities of TFIIH. Both TFIIH and TFIIE are required for promoter clearance by RNA polymerase.
KEGG Pathway
Basal transcription factors (hsa03022 )
Viral carcinogenesis (hsa05203 )
Reactome Pathway
RNA Polymerase II HIV Promoter Escape (R-HSA-167162 )
Transcription of the HIV genome (R-HSA-167172 )
RNA Polymerase II Pre-transcription Events (R-HSA-674695 )
RNA polymerase II transcribes snRNA genes (R-HSA-6807505 )
RNA Polymerase II Promoter Escape (R-HSA-73776 )
RNA Polymerase II Transcription Pre-Initiation And Promoter Opening (R-HSA-73779 )
RNA Polymerase II Transcription Initiation (R-HSA-75953 )
RNA Polymerase II Transcription Initiation And Promoter Clearance (R-HSA-76042 )
HIV Transcription Initiation (R-HSA-167161 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
6 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate affects the expression of General transcription factor IIE subunit 1 (GTF2E1). [1]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate decreases the expression of General transcription factor IIE subunit 1 (GTF2E1). [3]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of General transcription factor IIE subunit 1 (GTF2E1). [4]
Benzatropine DMF7EXL Approved Benzatropine decreases the expression of General transcription factor IIE subunit 1 (GTF2E1). [5]
Haloperidol DM96SE0 Approved Haloperidol decreases the expression of General transcription factor IIE subunit 1 (GTF2E1). [5]
Formaldehyde DM7Q6M0 Investigative Formaldehyde decreases the expression of General transcription factor IIE subunit 1 (GTF2E1). [7]
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⏷ Show the Full List of 6 Drug(s)
2 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin decreases the methylation of General transcription factor IIE subunit 1 (GTF2E1). [2]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 decreases the phosphorylation of General transcription factor IIE subunit 1 (GTF2E1). [6]
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References

1 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.
2 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
3 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
4 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
5 Cannabidiol Displays Proteomic Similarities to Antipsychotics in Cuprizone-Exposed Human Oligodendrocytic Cell Line MO3.13. Front Mol Neurosci. 2021 May 28;14:673144. doi: 10.3389/fnmol.2021.673144. eCollection 2021.
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.
7 Gene expression changes in primary human nasal epithelial cells exposed to formaldehyde in vitro. Toxicol Lett. 2010 Oct 5;198(2):289-95.