Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTUN0OAY)

DOT Name Phosphatase and actin regulator 3 (PHACTR3)
Synonyms Scaffold-associated PP1-inhibiting protein; Scapinin
Gene Name PHACTR3
Related Disease
Colorectal carcinoma ( )
Rheumatoid arthritis ( )
Schizophrenia ( )
UniProt ID
PHAR3_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Pfam ID
PF02755
Sequence
MAASEDGSGCLVSRGRSQSDPSVLTDSSATSSADAGENPDEMDQTPPARPEYLVSGIRTP
PVRRNSKLATLGRIFKPWKWRKKKNEKLKQTTSALEKKMAGRQGREELIKKGLLEMMEQD
AESKTCNPDGGPRSVQSEPPTPKSETLTSEDAQPGSPLATGTDQVSLDKPLSSAAHLDDA
AKMPSASSGEEADAGSLLPTTNELSQALAGADSLDSPPRPLERSVGQLPSPPLLPTPPPK
ASSKTTKNVTGQATLFQASSMKSADPSLRGQLSTPTGSPHLTTVHRPLPPSRVIEELHRA
LATKHRQDSFQGRESKGSPKKRLDVRLSRTSSVERGKEREEAWSFDGALENKRTAAKESE
ENKENLIINSELKDDLLLYQDEEALNDSIISGTLPRKCKKELLAVKLRNRPSKQELEDRN
IFPRRTDEERQEIRQQIEMKLSKRLSQRPAVEELERRNILKQRNDQTEQEERREIKQRLT
RKLNQRPTVDELRDRKILIRFSDYVEVAKAQDYDRRADKPWTRLSAADKAAIRKELNEYK
SNEMEVHASSKHLTRFHRP
Tissue Specificity Abundantly expressed in brain. Also found in several tumors such as lung carcinomas, nervous tumors and HL-60 leukemia cells. Isoform 3 is the major form in U-937, GOTO and HL-60 leukemia cells.

Molecular Interaction Atlas (MIA) of This DOT

3 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Colorectal carcinoma DIS5PYL0 Definitive Posttranslational Modification [1]
Rheumatoid arthritis DISTSB4J Strong Genetic Variation [2]
Schizophrenia DISSRV2N Strong Genetic Variation [3]
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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 Phosphatase and actin regulator 3 (PHACTR3). [4]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the methylation of Phosphatase and actin regulator 3 (PHACTR3). [6]
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5 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Triclosan DMZUR4N Approved Triclosan decreases the expression of Phosphatase and actin regulator 3 (PHACTR3). [5]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Phosphatase and actin regulator 3 (PHACTR3). [7]
Leflunomide DMR8ONJ Phase 1 Trial Leflunomide increases the expression of Phosphatase and actin regulator 3 (PHACTR3). [8]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Phosphatase and actin regulator 3 (PHACTR3). [9]
Formaldehyde DM7Q6M0 Investigative Formaldehyde decreases the expression of Phosphatase and actin regulator 3 (PHACTR3). [10]
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References

1 DNA methylation of phosphatase and actin regulator 3 detects colorectal cancer in stool and complements FIT.Cancer Prev Res (Phila). 2012 Mar;5(3):464-72. doi: 10.1158/1940-6207.CAPR-11-0315. Epub 2011 Dec 1.
2 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.
3 Genome-wide association analysis identifies 30 new susceptibility loci for schizophrenia.Nat Genet. 2017 Nov;49(11):1576-1583. doi: 10.1038/ng.3973. Epub 2017 Oct 9.
4 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.
5 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
6 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.
7 CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.
8 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
9 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.
10 Gene expression changes in primary human nasal epithelial cells exposed to formaldehyde in vitro. Toxicol Lett. 2010 Oct 5;198(2):289-95.