Details of Drug Off-Target (DOT)

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

DOT Name Rho guanine nucleotide exchange factor 37 (ARHGEF37)
Gene Name ARHGEF37
UniProt ID
ARH37_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Pfam ID
PF00621 ; PF00018 ; PF07653
Sequence
MAKHGADEPSSRSGSPDREGRASEDRSLLHQRLAVRELIDTEVSYLHMLQLCASDIRSRL
QQLPQGDLDVLFSNIDDIIKVNSRFLHDLQETASKEEEQVQLVGNIFLEFQEELEQVYKV
YCASYDQALLLVDTYRKEPELQRHIQGIVEAVVPQAGSSGLSFLLVIPLQRITRYPLLLQ
KILENTVPDASAYPVLQRAVSALQDVNTNINEYKMRKEVASKYTKVEQLTLRERLARINT
HTLSKKTTRLSQLLKQEAGLIPRTEDKEFDDLEERFQWVSLCVTELKNNVAAYLDNLQAF
LYFRPHEYNLDIPEGPAVQYCNLARDLHLEAFLKFKQRLEGLVWQPLCSLAKALLGPQNL
IKKRLDKLLDFERVEEKLLEVGSVTYQEEAARHTYQALNSLLVAELPQFNQLVMQWLGQI
MCTFVTLQRDLAKQVLQRAEGSMAQLPHHHVPEPAFRKLVEDALGRTSNQLRSFQETFEK
VQPPPTTQPLLPGSERQVQALLSRYGPGKLYQVTSNISGTGTLDLTLPRGQIVAILQNKD
TKGNSGRWLVDTGGHRGYVPAGKLQLYHVVPSAEELRRQAGLNKDPRCLTPEPSPALVPS
IPTMNQVIAAYPFVARSSHEVSLQAGQPVTILEAQDKKGNPEWSLVEVNGQRGYVPSGFL
ARARSPVLWGWSLPS
Function May act as a guanine nucleotide exchange factor (GEF).
Reactome Pathway
G alpha (12/13) signalling events (R-HSA-416482 )
NRAGE signals death through JNK (R-HSA-193648 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
10 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 Rho guanine nucleotide exchange factor 37 (ARHGEF37). [1]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [2]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [3]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [4]
Testosterone DM7HUNW Approved Testosterone increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [4]
Triclosan DMZUR4N Approved Triclosan increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [5]
SNDX-275 DMH7W9X Phase 3 SNDX-275 increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [6]
Belinostat DM6OC53 Phase 2 Belinostat decreases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [7]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [9]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [11]
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⏷ Show the Full List of 10 Drug(s)
2 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene affects the methylation of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [8]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of Rho guanine nucleotide exchange factor 37 (ARHGEF37). [10]
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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 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
3 17-Estradiol Activates HSF1 via MAPK Signaling in ER-Positive Breast Cancer Cells. Cancers (Basel). 2019 Oct 11;11(10):1533. doi: 10.3390/cancers11101533.
4 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
5 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
6 Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
7 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
8 Effect of aflatoxin B(1), benzo[a]pyrene, and methapyrilene on transcriptomic and epigenetic alterations in human liver HepaRG cells. Food Chem Toxicol. 2018 Nov;121:214-223. doi: 10.1016/j.fct.2018.08.034. Epub 2018 Aug 26.
9 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.
10 DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.
11 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.