Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTYZ1NV8)

DOT Name Rhophilin-1 (RHPN1)
Synonyms GTP-Rho-binding protein 1
Gene Name RHPN1
Related Disease
Advanced cancer ( )
Breast cancer ( )
Breast carcinoma ( )
Polycystic ovarian syndrome ( )
Uveal Melanoma ( )
Head-neck squamous cell carcinoma ( )
Neoplasm ( )
UniProt ID
RHPN1_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Pfam ID
PF03097 ; PF02185 ; PF00595
Sequence
MILEERPDGAGAGEESPRLQGCDSLTQIQCGQLQSRRAQIHQQIDKELQMRTGAENLYRA
TSNNRVRETVALELSYVNSNLQLLKEELEELSGGVDPGRHGSEAVTVPMIPLGLKETKEL
DWSTPLKELISVHFGEDGASYEAEIRELEALRQAMRTPSRNESGLELLTAYYNQLCFLDA
RFLTPARSLGLFFHWYDSLTGVPAQQRALAFEKGSVLFNIGALHTQIGARQDRSCTEGAR
RAMEAFQRAAGAFSLLRENFSHAPSPDMSAASLCALEQLMMAQAQECVFEGLSPPASMAP
QDCLAQLRLAQEAAQVAAEYRLVHRTMAQPPVHDYVPVSWTALVHVKAEYFRSLAHYHVA
MALCDGSPATEGELPTHEQVFLQPPTSSKPRGPVLPQELEERRQLGKAHLKRAILGQEEA
LRLHALCRVLREVDLLRAVISQTLQRSLAKYAELDREDDFCEAAEAPDIQPKTHQKPEAR
MPRLSQGKGPDIFHRLGPLSVFSAKNRWRLVGPVHLTRGEGGFGLTLRGDSPVLIAAVIP
GSQAAAAGLKEGDYIVSVNGQPCRWWRHAEVVTELKAAGEAGASLQVVSLLPSSRLPSLG
DRRPVLLGPRGLLRSQREHGCKTPASTWASPRPLLNWSRKAQQGKTGGCPQPCAPVKPAP
PSSLKHPGWP
Function Has no enzymatic activity. May serve as a target for Rho, and interact with some cytoskeletal component upon Rho binding or relay a Rho signal to other molecules.
Reactome Pathway
RHOA GTPase cycle (R-HSA-8980692 )
RHO GTPases Activate Rhotekin and Rhophilins (R-HSA-5666185 )

Molecular Interaction Atlas (MIA) of This DOT

7 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Advanced cancer DISAT1Z9 Strong Biomarker [1]
Breast cancer DIS7DPX1 Strong Biomarker [2]
Breast carcinoma DIS2UE88 Strong Biomarker [2]
Polycystic ovarian syndrome DISZ2BNG Strong Biomarker [3]
Uveal Melanoma DISA7ZGL Strong Biomarker [4]
Head-neck squamous cell carcinoma DISF7P24 moderate Biomarker [5]
Neoplasm DISZKGEW moderate Altered Expression [5]
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⏷ Show the Full List of 7 Disease(s)
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 Rhophilin-1 (RHPN1). [6]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the methylation of Rhophilin-1 (RHPN1). [7]
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3 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Rhophilin-1 (RHPN1). [8]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Rhophilin-1 (RHPN1). [9]
Sulforaphane DMQY3L0 Investigative Sulforaphane decreases the expression of Rhophilin-1 (RHPN1). [10]
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References

1 Co-expression of key gene modules and pathways of human breast cancer cell lines.Biosci Rep. 2019 Jul 18;39(7):BSR20181925. doi: 10.1042/BSR20181925. Print 2019 Jul 31.
2 c-Myc induced the regulation of long non-coding RNA RHPN1-AS1 on breast cancer cell proliferation via inhibiting P53.Mol Genet Genomics. 2019 Oct;294(5):1219-1229. doi: 10.1007/s00438-019-01572-w. Epub 2019 May 14.
3 Progesterone resistance in PCOS endometrium: a microarray analysis in clomiphene citrate-treated and artificial menstrual cycles.J Clin Endocrinol Metab. 2011 Jun;96(6):1737-46. doi: 10.1210/jc.2010-2600. Epub 2011 Mar 16.
4 The Long Non-Coding RNA RHPN1-AS1 Promotes Uveal Melanoma Progression.Int J Mol Sci. 2017 Jan 23;18(1):226. doi: 10.3390/ijms18010226.
5 Knockdown of LncRNA RHPN1-AS1 Inhibits Cell Migration, Invasion and Proliferation in Head and Neck Squamous Cell Carcinoma.J Cancer. 2019 Jul 5;10(17):4000-4008. doi: 10.7150/jca.29029. eCollection 2019.
6 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.
7 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.
8 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.
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 Transcriptome and DNA methylation changes modulated by sulforaphane induce cell cycle arrest, apoptosis, DNA damage, and suppression of proliferation in human liver cancer cells. Food Chem Toxicol. 2020 Feb;136:111047. doi: 10.1016/j.fct.2019.111047. Epub 2019 Dec 12.