General Information of Drug Off-Target (DOT) (ID: OT4T2BS1)

DOT Name Insulin-like growth factor-binding protein 3 receptor (TMEM219)
Synonyms IGFBP-3R; Transmembrane protein 219
Gene Name TMEM219
UniProt ID
TM219_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Pfam ID
PF14940
Sequence
MGNCQAGHNLHLCLAHHPPLVCATLILLLLGLSGLGLGSFLLTHRTGLRSPDIPQDWVSF
LRSFGQLTLCPRNGTVTGKWRGSHVVGLLTTLNFGDGPDRNKTRTFQATVLGSQMGLKGS
SAGQLVLITARVTTERTAGTCLYFSAVPGILPSSQPPISCSEEGAGNATLSPRMGEECVS
VWSHEGLVLTKLLTSEELALCGSRLLVLGSFLLLFCGLLCCVTAMCFHPRRESHWSRTRL
Function Cell death receptor specific for IGFBP3, may mediate caspase-8-dependent apoptosis upon ligand binding.
Tissue Specificity Widely expressed in normal tissues but suppressed in prostate and breast tumor.
Reactome Pathway
TP53 Regulates Transcription of Death Receptors and Ligands (R-HSA-6803211 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
2 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of Insulin-like growth factor-binding protein 3 receptor (TMEM219). [1]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the methylation of Insulin-like growth factor-binding protein 3 receptor (TMEM219). [5]
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4 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 Insulin-like growth factor-binding protein 3 receptor (TMEM219). [2]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Insulin-like growth factor-binding protein 3 receptor (TMEM219). [3]
Temozolomide DMKECZD Approved Temozolomide decreases the expression of Insulin-like growth factor-binding protein 3 receptor (TMEM219). [4]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Insulin-like growth factor-binding protein 3 receptor (TMEM219). [6]
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References

1 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
2 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
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 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 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
6 Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells. J Biol Chem. 2012 Dec 14;287(51):43137-55.