General Information of Drug Off-Target (DOT) (ID: OT2UGZA9)

DOT Name CD63 antigen (CD63)
Synonyms
Granulophysin; Lysosomal-associated membrane protein 3; LAMP-3; Lysosome integral membrane protein 1; Limp1; Melanoma-associated antigen ME491; OMA81H; Ocular melanoma-associated antigen; Tetraspanin-30; Tspan-30; CD antigen CD63
Gene Name CD63
Related Disease
Melanoma ( )
Acute myelogenous leukaemia ( )
Advanced cancer ( )
Alzheimer disease ( )
Astrocytoma ( )
Bone osteosarcoma ( )
Breast cancer ( )
Breast carcinoma ( )
Breast neoplasm ( )
Carcinoma of esophagus ( )
Colon cancer ( )
Colon carcinoma ( )
Esophageal cancer ( )
Esophageal squamous cell carcinoma ( )
Essential thrombocythemia ( )
Glioblastoma multiforme ( )
Hantavirus infection ( )
Hepatitis C virus infection ( )
Hermansky-Pudlak syndrome ( )
Liver cirrhosis ( )
Matthew-Wood syndrome ( )
Metastatic malignant neoplasm ( )
Nasopharyngeal carcinoma ( )
Neoplasm of esophagus ( )
Non-small-cell lung cancer ( )
Osteosarcoma ( )
Ovarian neoplasm ( )
Polycythemia vera ( )
Systemic lupus erythematosus ( )
Thyroid gland carcinoma ( )
Thyroid gland papillary carcinoma ( )
Thyroid tumor ( )
Urticaria ( )
Venous thromboembolism ( )
Carcinoma ( )
Colorectal carcinoma ( )
Type-1 diabetes ( )
Adenocarcinoma ( )
Adult glioblastoma ( )
Asthma ( )
Chronic obstructive pulmonary disease ( )
Gastric cancer ( )
Neoplasm ( )
Prostate cancer ( )
Prostate carcinoma ( )
Rheumatoid arthritis ( )
Stomach cancer ( )
UniProt ID
CD63_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Pfam ID
PF00335
Sequence
MAVEGGMKCVKFLLYVLLLAFCACAVGLIAVGVGAQLVLSQTIIQGATPGSLLPVVIIAV
GVFLFLVAFVGCCGACKENYCLMITFAIFLSLIMLVEVAAAIAGYVFRDKVMSEFNNNFR
QQMENYPKNNHTASILDRMQADFKCCGAANYTDWEKIPSMSKNRVPDSCCINVTVGCGIN
FNEKAIHKEGCVEKIGGWLRKNVLVVAAAALGIAFVEVLGIVFACCLVKSIRSGYEVM
Function
Functions as a cell surface receptor for TIMP1 and plays a role in the activation of cellular signaling cascades. Plays a role in the activation of ITGB1 and integrin signaling, leading to the activation of AKT, FAK/PTK2 and MAP kinases. Promotes cell survival, reorganization of the actin cytoskeleton, cell adhesion, spreading and migration, via its role in the activation of AKT and FAK/PTK2. Plays a role in VEGFA signaling via its role in regulating the internalization of KDR/VEGFR2. Plays a role in intracellular vesicular transport processes, and is required for normal trafficking of the PMEL luminal domain that is essential for the development and maturation of melanocytes. Plays a role in the adhesion of leukocytes onto endothelial cells via its role in the regulation of SELP trafficking. May play a role in mast cell degranulation in response to Ms4a2/FceRI stimulation, but not in mast cell degranulation in response to other stimuli.
Tissue Specificity Detected in platelets (at protein level). Dysplastic nevi, radial growth phase primary melanomas, hematopoietic cells, tissue macrophages.
KEGG Pathway
Lysosome (hsa04142 )
Proteoglycans in cancer (hsa05205 )
Reactome Pathway
Neutrophil degranulation (R-HSA-6798695 )
Platelet degranulation (R-HSA-114608 )

Molecular Interaction Atlas (MIA) of This DOT

47 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Melanoma DIS1RRCY Definitive Biomarker [1]
Acute myelogenous leukaemia DISCSPTN Strong Biomarker [2]
Advanced cancer DISAT1Z9 Strong Biomarker [3]
Alzheimer disease DISF8S70 Strong Biomarker [4]
Astrocytoma DISL3V18 Strong Biomarker [5]
Bone osteosarcoma DIST1004 Strong Altered Expression [6]
Breast cancer DIS7DPX1 Strong Biomarker [7]
Breast carcinoma DIS2UE88 Strong Biomarker [7]
Breast neoplasm DISNGJLM Strong Altered Expression [8]
Carcinoma of esophagus DISS6G4D Strong Altered Expression [9]
Colon cancer DISVC52G Strong Altered Expression [10]
Colon carcinoma DISJYKUO Strong Altered Expression [10]
Esophageal cancer DISGB2VN Strong Altered Expression [9]
Esophageal squamous cell carcinoma DIS5N2GV Strong Biomarker [11]
Essential thrombocythemia DISWWK11 Strong Altered Expression [12]
Glioblastoma multiforme DISK8246 Strong Altered Expression [5]
Hantavirus infection DISZFTMH Strong Biomarker [13]
Hepatitis C virus infection DISQ0M8R Strong Biomarker [14]
Hermansky-Pudlak syndrome DISCY0HQ Strong Biomarker [15]
Liver cirrhosis DIS4G1GX Strong Biomarker [16]
Matthew-Wood syndrome DISA7HR7 Strong Biomarker [17]
Metastatic malignant neoplasm DIS86UK6 Strong Altered Expression [18]
Nasopharyngeal carcinoma DISAOTQ0 Strong Biomarker [19]
Neoplasm of esophagus DISOLKAQ Strong Altered Expression [9]
Non-small-cell lung cancer DIS5Y6R9 Strong Biomarker [20]
Osteosarcoma DISLQ7E2 Strong Altered Expression [6]
Ovarian neoplasm DISEAFTY Strong Altered Expression [21]
Polycythemia vera DISB5FPO Strong Biomarker [22]
Systemic lupus erythematosus DISI1SZ7 Strong Biomarker [23]
Thyroid gland carcinoma DISMNGZ0 Strong Altered Expression [18]
Thyroid gland papillary carcinoma DIS48YMM Strong Genetic Variation [24]
Thyroid tumor DISLVKMD Strong Biomarker [18]
Urticaria DIS9WQAI Strong Biomarker [25]
Venous thromboembolism DISUR7CR Strong Biomarker [26]
Carcinoma DISH9F1N moderate Altered Expression [27]
Colorectal carcinoma DIS5PYL0 moderate Biomarker [28]
Type-1 diabetes DIS7HLUB moderate Biomarker [29]
Adenocarcinoma DIS3IHTY Limited Biomarker [30]
Adult glioblastoma DISVP4LU Limited Biomarker [5]
Asthma DISW9QNS Limited Biomarker [31]
Chronic obstructive pulmonary disease DISQCIRF Limited Altered Expression [32]
Gastric cancer DISXGOUK Limited Biomarker [33]
Neoplasm DISZKGEW Limited Biomarker [11]
Prostate cancer DISF190Y Limited Biomarker [34]
Prostate carcinoma DISMJPLE Limited Biomarker [34]
Rheumatoid arthritis DISTSB4J Limited Biomarker [35]
Stomach cancer DISKIJSX Limited Biomarker [33]
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⏷ Show the Full List of 47 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
21 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 CD63 antigen (CD63). [36]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of CD63 antigen (CD63). [37]
Tretinoin DM49DUI Approved Tretinoin increases the expression of CD63 antigen (CD63). [38]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of CD63 antigen (CD63). [39]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of CD63 antigen (CD63). [40]
Cisplatin DMRHGI9 Approved Cisplatin affects the expression of CD63 antigen (CD63). [41]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of CD63 antigen (CD63). [42]
Quercetin DM3NC4M Approved Quercetin increases the expression of CD63 antigen (CD63). [43]
Temozolomide DMKECZD Approved Temozolomide decreases the expression of CD63 antigen (CD63). [44]
Fluorouracil DMUM7HZ Approved Fluorouracil decreases the expression of CD63 antigen (CD63). [45]
Dasatinib DMJV2EK Approved Dasatinib decreases the expression of CD63 antigen (CD63). [46]
Clozapine DMFC71L Approved Clozapine increases the expression of CD63 antigen (CD63). [47]
Diphenylpyraline DMW4X37 Approved Diphenylpyraline increases the expression of CD63 antigen (CD63). [46]
Asasantin DMCZIHT Approved Asasantin decreases the expression of CD63 antigen (CD63). [48]
Tocopherol DMBIJZ6 Phase 2 Tocopherol increases the expression of CD63 antigen (CD63). [49]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of CD63 antigen (CD63). [52]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of CD63 antigen (CD63). [53]
chloropicrin DMSGBQA Investigative chloropicrin decreases the expression of CD63 antigen (CD63). [54]
Glyphosate DM0AFY7 Investigative Glyphosate decreases the expression of CD63 antigen (CD63). [55]
Phencyclidine DMQBEYX Investigative Phencyclidine decreases the expression of CD63 antigen (CD63). [56]
Fmet-leu-phe DMQ391A Investigative Fmet-leu-phe increases the expression of CD63 antigen (CD63). [57]
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⏷ Show the Full List of 21 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 increases the methylation of CD63 antigen (CD63). [50]
TAK-243 DM4GKV2 Phase 1 TAK-243 increases the sumoylation of CD63 antigen (CD63). [51]
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References

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2 Leukemia-derived exosomes induced IL-8 production in bone marrow stromal cells to protect the leukemia cells against chemotherapy.Life Sci. 2019 Mar 15;221:187-195. doi: 10.1016/j.lfs.2019.02.003. Epub 2019 Feb 2.
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6 Ameloblastin induces tumor suppressive phenotype and enhances chemosensitivity to doxorubicin via Src-Stat3 inactivation in osteosarcoma.Sci Rep. 2017 Jan 5;7:40187. doi: 10.1038/srep40187.
7 Novel breast cancer screening: combined expression of miR-21 and MMP-1 in urinary exosomes detects 95% of breast cancer without metastasis.Sci Rep. 2019 Sep 19;9(1):13595. doi: 10.1038/s41598-019-50084-5.
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10 Disruption of Core 1-mediated O-glycosylation oppositely regulates CD44 expression in human colon cancer cells and tumor-derived exosomes.Biochem Biophys Res Commun. 2020 Jan 8;521(2):514-520. doi: 10.1016/j.bbrc.2019.10.149. Epub 2019 Oct 31.
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21 Expression and significance of the protein and mRNA of metastasis suppressor gene ME491/CD63 and integrin alpha5 in ovarian cancer tissues.Eur J Gynaecol Oncol. 2007;28(3):179-83.
22 Phosphoproteomic Landscaping Identifies Non-canonical cKIT Signaling in Polycythemia Vera Erythroid Progenitors.Front Oncol. 2019 Nov 22;9:1245. doi: 10.3389/fonc.2019.01245. eCollection 2019.
23 Contribution and underlying mechanisms of CXCR4 overexpression in patients with systemic lupus erythematosus.Cell Mol Immunol. 2017 Oct;14(10):842-849. doi: 10.1038/cmi.2016.47. Epub 2016 Sep 26.
24 BRAFV600E mutation, TIMP-1 upregulation, and NF-B activation: closing the loop on the papillary thyroid cancer trilogy.Endocr Relat Cancer. 2011 Nov 14;18(6):669-85. doi: 10.1530/ERC-11-0076. Print 2011 Dec.
25 Basophil CD63 expression in chronic spontaneous urticaria: correlation with allergic sensitization, serum autoreactivity and basophil reactivity.J Eur Acad Dermatol Venereol. 2017 Mar;31(3):463-468. doi: 10.1111/jdv.13912. Epub 2016 Sep 5.
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27 Down-regulation of TM4SF is associated with the metastatic potential of gastric carcinoma TM4SF members in gastric carcinoma.World J Surg Oncol. 2011 Apr 27;9:43. doi: 10.1186/1477-7819-9-43.
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31 Cultured mast cells from patients with asthma and controls respond with similar sensitivity to recombinant Der p2-induced, IgE-mediated activation.Scand J Immunol. 2013 Oct;78(4):352-6. doi: 10.1111/sji.12085.
32 PMN degranulation in relation to CD63 expression and genetic polymorphisms in healthy individuals and COPD patients.Int J Mol Med. 2007 May;19(5):817-22. doi: 10.3892/ijmm.19.5.817.
33 Clinico-pathological significance of exosome marker CD63 expression on cancer cells and stromal cells in gastric cancer.PLoS One. 2018 Sep 17;13(9):e0202956. doi: 10.1371/journal.pone.0202956. eCollection 2018.
34 Nanoscale flow cytometry to distinguish subpopulations of prostate extracellular vesicles in patient plasma.Prostate. 2019 May;79(6):592-603. doi: 10.1002/pros.23764. Epub 2019 Jan 24.
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38 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
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42 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
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