Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT8TKE6F)

DOT Name G-protein coupled receptor 78 (GPR78)
Gene Name GPR78
Related Disease
Bipolar disorder ( )
Lung squamous cell carcinoma ( )
Schizophrenia ( )
Lewy body dementia ( )
Lung cancer ( )
Lung carcinoma ( )
Neuroblastoma ( )
Parkinson disease ( )
UniProt ID
GPR78_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Pfam ID
PF00001
Sequence
MGPGEALLAGLLVMVLAVALLSNALVLLCCAYSAELRTRASGVLLVNLSLGHLLLAALDM
PFTLLGVMRGRTPSAPGACQVIGFLDTFLASNAALSVAALSADQWLAVGFPLRYAGRLRP
RYAGLLLGCAWGQSLAFSGAALGCSWLGYSSAFASCSLRLPPEPERPRFAAFTATLHAVG
FVLPLAVLCLTSLQVHRVARRHCQRMDTVTMKALALLADLHPSVRQRCLIQQKRRRHRAT
RKIGIAIATFLICFAPYVMTRLAELVPFVTVNAQWGILSKCLTYSKAVADPFTYSLLRRP
FRQVLAGMVHRLLKRTPRPASTHDSSLDVAGMVHQLLKRTPRPASTHNGSVDTENDSCLQ
QTH
Function Orphan receptor. Displays a significant level of constitutive activity. Its effect is mediated by G(s)-alpha protein that stimulate adenylate cyclase, resulting in an elevation of intracellular cAMP.
Tissue Specificity High level of expression in placenta. Expressed throughout the brain at low level. No expression detected in skeletal muscle, lung, heart, liver, pancreas, or kidney.

Molecular Interaction Atlas (MIA) of This DOT

8 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Bipolar disorder DISAM7J2 Strong Biomarker [1]
Lung squamous cell carcinoma DISXPIBD Strong Biomarker [2]
Schizophrenia DISSRV2N Strong Biomarker [1]
Lewy body dementia DISAE66J Limited Altered Expression [3]
Lung cancer DISCM4YA Limited Biomarker [4]
Lung carcinoma DISTR26C Limited Biomarker [4]
Neuroblastoma DISVZBI4 Limited Genetic Variation [5]
Parkinson disease DISQVHKL Limited Altered Expression [3]
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⏷ Show the Full List of 8 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
4 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of G-protein coupled receptor 78 (GPR78). [6]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of G-protein coupled receptor 78 (GPR78). [7]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of G-protein coupled receptor 78 (GPR78). [8]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of G-protein coupled receptor 78 (GPR78). [10]
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1 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 increases the methylation of G-protein coupled receptor 78 (GPR78). [9]
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References

1 Association analysis of the chromosome 4p-located G protein-coupled receptor 78 (GPR78) gene in bipolar affective disorder and schizophrenia.Mol Psychiatry. 2006 Apr;11(4):384-94. doi: 10.1038/sj.mp.4001786.
2 Predicting the Lung Squamous Cell Carcinoma Diagnosis and Prognosis Markers by Unique DNA Methylation and Gene Expression Profiles.J Comput Biol. 2020 Jul;27(7):1041-1054. doi: 10.1089/cmb.2019.0138. Epub 2019 Nov 11.
3 GRP78 Level Is Altered in the Brain, but Not in Plasma or Cerebrospinal Fluid in Parkinson's Disease Patients.Front Neurosci. 2019 Jul 5;13:697. doi: 10.3389/fnins.2019.00697. eCollection 2019.
4 GPR78 promotes lung cancer cell migration and metastasis by activation of Gq-Rho GTPase pathway.BMB Rep. 2016 Nov;49(11):623-628. doi: 10.5483/bmbrep.2016.49.11.133.
5 Common variants upstream of MLF1 at 3q25 and within CPZ at 4p16 associated with neuroblastoma.PLoS Genet. 2017 May 18;13(5):e1006787. doi: 10.1371/journal.pgen.1006787. eCollection 2017 May.
6 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
7 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.
8 Endoplasmic reticulum stress contributes to arsenic trioxide-induced intrinsic apoptosis in human umbilical and bone marrow mesenchymal stem cells. Environ Toxicol. 2016 Mar;31(3):314-28.
9 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.
10 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.