General Information of Drug Off-Target (DOT) (ID: OTUZ3U9Z)

DOT Name Cdc42 effector protein 3 (CDC42EP3)
Synonyms Binder of Rho GTPases 2; MSE55-related Cdc42-binding protein
Gene Name CDC42EP3
Related Disease
Neoplasm ( )
Uveal Melanoma ( )
Bladder cancer ( )
Breast cancer ( )
Esophageal squamous cell carcinoma ( )
Lung cancer ( )
Lung carcinoma ( )
Rheumatoid arthritis ( )
Schizophrenia ( )
Transitional cell carcinoma ( )
Urinary bladder cancer ( )
Urinary bladder neoplasm ( )
Urothelial carcinoma ( )
Squamous cell carcinoma ( )
Adenocarcinoma ( )
UniProt ID
BORG2_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Pfam ID
PF14957 ; PF00786
Sequence
MPAKTPIYLKAANNKKGKKFKLRDILSPDMISPPLGDFRHTIHIGKEGQHDVFGDISFLQ
GNYELLPGNQEKAHLGQFPGHNEFFRANSTSDSVFTETPSPVLKNAISLPTIGGSQALML
PLLSPVTFNSKQESFGPAKLPRLSCEPVMEEKAQEKSSLLENGTVHQGDTSWGSSGSASQ
SSQGRDSHSSSLSEQYPDWPAEDMFDHPTPCELIKGKTKSEESLSDLTGSLLSLQLDLGP
SLLDEVLNVMDKNK
Function
Probably involved in the organization of the actin cytoskeleton. May act downstream of CDC42 to induce actin filament assembly leading to cell shape changes. Induces pseudopodia formation in fibroblasts.
Tissue Specificity Highly expressed in the heart and weakly in the brain.
Reactome Pathway
CDC42 GTPase cycle (R-HSA-9013148 )
RHOQ GTPase cycle (R-HSA-9013406 )
MAPK6/MAPK4 signaling (R-HSA-5687128 )

Molecular Interaction Atlas (MIA) of This DOT

15 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Neoplasm DISZKGEW Definitive Biomarker [1]
Uveal Melanoma DISA7ZGL Definitive Genetic Variation [2]
Bladder cancer DISUHNM0 Strong Biomarker [3]
Breast cancer DIS7DPX1 Strong Biomarker [4]
Esophageal squamous cell carcinoma DIS5N2GV Strong Biomarker [5]
Lung cancer DISCM4YA Strong Biomarker [6]
Lung carcinoma DISTR26C Strong Biomarker [6]
Rheumatoid arthritis DISTSB4J Strong Genetic Variation [7]
Schizophrenia DISSRV2N Strong Biomarker [8]
Transitional cell carcinoma DISWVVDR Strong Biomarker [9]
Urinary bladder cancer DISDV4T7 Strong Biomarker [3]
Urinary bladder neoplasm DIS7HACE Strong Biomarker [3]
Urothelial carcinoma DISRTNTN Strong Biomarker [9]
Squamous cell carcinoma DISQVIFL moderate Biomarker [10]
Adenocarcinoma DIS3IHTY Limited Biomarker [11]
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⏷ Show the Full List of 15 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
22 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of Cdc42 effector protein 3 (CDC42EP3). [12]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [13]
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [14]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Cdc42 effector protein 3 (CDC42EP3). [15]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [16]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Cdc42 effector protein 3 (CDC42EP3). [17]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Cdc42 effector protein 3 (CDC42EP3). [18]
Testosterone DM7HUNW Approved Testosterone increases the expression of Cdc42 effector protein 3 (CDC42EP3). [18]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Cdc42 effector protein 3 (CDC42EP3). [19]
Marinol DM70IK5 Approved Marinol decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [20]
Phenobarbital DMXZOCG Approved Phenobarbital affects the expression of Cdc42 effector protein 3 (CDC42EP3). [21]
Progesterone DMUY35B Approved Progesterone increases the expression of Cdc42 effector protein 3 (CDC42EP3). [22]
Panobinostat DM58WKG Approved Panobinostat decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [23]
Ethinyl estradiol DMODJ40 Approved Ethinyl estradiol affects the expression of Cdc42 effector protein 3 (CDC42EP3). [24]
Melphalan DMOLNHF Approved Melphalan decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [25]
Urethane DM7NSI0 Phase 4 Urethane increases the expression of Cdc42 effector protein 3 (CDC42EP3). [26]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone increases the expression of Cdc42 effector protein 3 (CDC42EP3). [27]
Genistein DM0JETC Phase 2/3 Genistein affects the expression of Cdc42 effector protein 3 (CDC42EP3). [24]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [29]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of Cdc42 effector protein 3 (CDC42EP3). [31]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Cdc42 effector protein 3 (CDC42EP3). [32]
Milchsaure DM462BT Investigative Milchsaure increases the expression of Cdc42 effector protein 3 (CDC42EP3). [33]
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⏷ Show the Full List of 22 Drug(s)
3 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 decreases the methylation of Cdc42 effector protein 3 (CDC42EP3). [28]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of Cdc42 effector protein 3 (CDC42EP3). [30]
Coumarin DM0N8ZM Investigative Coumarin increases the phosphorylation of Cdc42 effector protein 3 (CDC42EP3). [34]
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References

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3 Automated quantification of FISH signals in urinary cells enables the assessment of chromosomal aberration patterns characteristic for bladder cancer.Biochem Biophys Res Commun. 2014 Jun 13;448(4):467-72. doi: 10.1016/j.bbrc.2014.04.137. Epub 2014 May 4.
4 FGD5 amplification in breast cancer patients is associated with tumour proliferation and a poorer prognosis.Breast Cancer Res Treat. 2017 Apr;162(2):243-253. doi: 10.1007/s10549-017-4125-8. Epub 2017 Jan 25.
5 Chromosomal aneuploidies and combinational fluorescence in situ hybridization probe panels are useful for predicting prognosis for esophageal squamous cell carcinoma.J Gastroenterol. 2015 Feb;50(2):155-66. doi: 10.1007/s00535-014-0961-z. Epub 2014 May 11.
6 Recurrent genomic gains in preinvasive lesions as a biomarker of risk for lung cancer.PLoS One. 2009 Jun 9;4(6):e5611. doi: 10.1371/journal.pone.0005611.
7 Studying the effects of haplotype partitioning methods on the RA-associated genomic results from the North American Rheumatoid Arthritis Consortium (NARAC) dataset.J Adv Res. 2019 Jan 18;18:113-126. doi: 10.1016/j.jare.2019.01.006. eCollection 2019 Jul.
8 Altered cortical CDC42 signaling pathways in schizophrenia: implications for dendritic spine deficits.Biol Psychiatry. 2010 Jul 1;68(1):25-32. doi: 10.1016/j.biopsych.2010.02.016. Epub 2010 Apr 10.
9 The development of a multitarget, multicolor fluorescence in situ hybridization assay for the detection of urothelial carcinoma in urine.J Mol Diagn. 2000 Aug;2(3):116-23. doi: 10.1016/S1525-1578(10)60625-3.
10 Analysis of the chromosomal aneuploidy by interphase fluorescence in situ hybridization (FISH) in Squamous cell carcinoma of the cervix in Jammu region of J and K state.J Cancer Res Ther. 2014 Apr-Jun;10(2):317-23. doi: 10.4103/0973-1482.136612.
11 A potential probe set of fluorescence in situ hybridization for detection of lung cancer in bronchial brushing specimens.J Cancer Res Clin Oncol. 2012 Sep;138(9):1541-9. doi: 10.1007/s00432-012-1232-0. Epub 2012 Apr 27.
12 Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
13 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.
14 Systems analysis of transcriptome and proteome in retinoic acid/arsenic trioxide-induced cell differentiation/apoptosis of promyelocytic leukemia. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7653-8.
15 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.
16 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.
17 Low doses of cisplatin induce gene alterations, cell cycle arrest, and apoptosis in human promyelocytic leukemia cells. Biomark Insights. 2016 Aug 24;11:113-21.
18 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
19 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.
20 Single-cell Transcriptome Mapping Identifies Common and Cell-type Specific Genes Affected by Acute Delta9-tetrahydrocannabinol in Humans. Sci Rep. 2020 Feb 26;10(1):3450. doi: 10.1038/s41598-020-59827-1.
21 Reproducible chemical-induced changes in gene expression profiles in human hepatoma HepaRG cells under various experimental conditions. Toxicol In Vitro. 2009 Apr;23(3):466-75. doi: 10.1016/j.tiv.2008.12.018. Epub 2008 Dec 30.
22 Progesterone regulation of implantation-related genes: new insights into the role of oestrogen. Cell Mol Life Sci. 2007 Apr;64(7-8):1009-32.
23 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.
24 Dose- and time-dependent transcriptional response of Ishikawa cells exposed to genistein. Toxicol Sci. 2016 May;151(1):71-87.
25 Bone marrow osteoblast damage by chemotherapeutic agents. PLoS One. 2012;7(2):e30758. doi: 10.1371/journal.pone.0030758. Epub 2012 Feb 17.
26 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
27 LSD1 activates a lethal prostate cancer gene network independently of its demethylase function. Proc Natl Acad Sci U S A. 2018 May 1;115(18):E4179-E4188.
28 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.
29 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.
30 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.
31 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.
32 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
33 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.
34 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.