Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T29879
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| Former ID |
TTDC00020
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| Target Name |
Integrin alpha-5
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| Gene Name |
ITGA5
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| Synonyms |
CD49e antigen; FNRA; Fibronectin receptor subunit alpha; Integrin alpha-5 heavy chain; Integrin alpha-5 light chain; Integrin alpha-F; VLA-5; ITGA5
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| Target Type |
Clinical Trial
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| Disease | Asthma [ICD10: J45] | ||||
| Allergy [ICD9: 995.3; ICD10: T78.4] | |||||
| Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | |||||
| Macular degeneration [ICD9: 362.5; ICD10: H35.3] | |||||
| Multiple scierosis [ICD9: 340; ICD10: G35] | |||||
| Function |
Integrin alpha-5/beta-1 is a receptor for fibronectin and fibrinogen. It recognizes the sequence R-G-D in its ligands. In case of HIV-1 infection, the interaction with extracellular viral Tat protein seems to enhance angiogenesis in Kaposi's sarcoma lesions.
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| BioChemical Class |
Integrin
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| Target Validation |
T29879
|
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| UniProt ID | |||||
| Sequence |
MGSRTPESPLHAVQLRWGPRRRPPLLPLLLLLLPPPPRVGGFNLDAEAPAVLSGPPGSFF
GFSVEFYRPGTDGVSVLVGAPKANTSQPGVLQGGAVYLCPWGASPTQCTPIEFDSKGSRL LESSLSSSEGEEPVEYKSLQWFGATVRAHGSSILACAPLYSWRTEKEPLSDPVGTCYLST DNFTRILEYAPCRSDFSWAAGQGYCQGGFSAEFTKTGRVVLGGPGSYFWQGQILSATQEQ IAESYYPEYLINLVQGQLQTRQASSIYDDSYLGYSVAVGEFSGDDTEDFVAGVPKGNLTY GYVTILNGSDIRSLYNFSGEQMASYFGYAVAATDVNGDGLDDLLVGAPLLMDRTPDGRPQ EVGRVYVYLQHPAGIEPTPTLTLTGHDEFGRFGSSLTPLGDLDQDGYNDVAIGAPFGGET QQGVVFVFPGGPGGLGSKPSQVLQPLWAASHTPDFFGSALRGGRDLDGNGYPDLIVGSFG VDKAVVYRGRPIVSASASLTIFPAMFNPEERSCSLEGNPVACINLSFCLNASGKHVADSI GFTVELQLDWQKQKGGVRRALFLASRQATLTQTLLIQNGAREDCREMKIYLRNESEFRDK LSPIHIALNFSLDPQAPVDSHGLRPALHYQSKSRIEDKAQILLDCGEDNICVPDLQLEVF GEQNHVYLGDKNALNLTFHAQNVGEGGAYEAELRVTAPPEAEYSGLVRHPGNFSSLSCDY FAVNQSRLLVCDLGNPMKAGASLWGGLRFTVPHLRDTKKTIQFDFQILSKNLNNSQSDVV SFRLSVEAQAQVTLNGVSKPEAVLFPVSDWHPRDQPQKEEDLGPAVHHVYELINQGPSSI SQGVLELSCPQALEGQQLLYVTRVTGLNCTTNHPINPKGLELDPEGSLHHQQKREAPSRS SASSGPQILKCPEAECFRLRCELGPLHQQESQSLQLHFRVWAKTFLQREHQPFSLQCEAV YKALKMPYRILPRQLPQKERQVATAVQWTKAEGSYGVPLWIIILAILFGLLLLGLLIYIL YKLGFFKRSLPYGTAMEKAQLKPPATSDA |
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| Structure |
3VI3; 3VI4; 4WJK; 4WK0; 4WK2; 4WK4
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| Drugs and Mode of Action | |||||
| Drug(s) | JSM 6427 | Drug Info | Phase 1 | Macular degeneration | [522128] |
| GW-559090 | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [547453] | |
| DW-908e | Drug Info | Discontinued in Phase 1 | Allergy | [547869] | |
| TR-14531 | Drug Info | Discontinued in Phase 1 | Asthma | [547054] | |
| ZD-7349 | Drug Info | Discontinued in Phase 1 | Multiple scierosis | [546708] | |
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Phagosome | ||||
| PI3K-Akt signaling pathway | |||||
| Focal adhesion | |||||
| ECM-receptor interaction | |||||
| Hematopoietic cell lineage | |||||
| Regulation of actin cytoskeleton | |||||
| Bacterial invasion of epithelial cells | |||||
| Shigellosis | |||||
| Pertussis | |||||
| Proteoglycans in cancer | |||||
| MicroRNAs in cancer | |||||
| Hypertrophic cardiomyopathy (HCM) | |||||
| Arrhythmogenic right ventricular cardiomyopathy (ARVC) | |||||
| Dilated cardiomyopathy | |||||
| NetPath Pathway | IL6 Signaling Pathway | ||||
| TNFalpha Signaling Pathway | |||||
| PANTHER Pathway | Integrin signalling pathway | ||||
| Pathway Interaction Database | Beta1 integrin cell surface interactions | ||||
| Integrin family cell surface interactions | |||||
| Arf6 trafficking events | |||||
| Angiopoietin receptor Tie2-mediated signaling | |||||
| CXCR4-mediated signaling events | |||||
| Plexin-D1 Signaling | |||||
| Syndecan-4-mediated signaling events | |||||
| Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
| Syndecan-2-mediated signaling events | |||||
| VEGFR3 signaling in lymphatic endothelium | |||||
| Signaling events mediated by focal adhesion kinase | |||||
| Reactome | Elastic fibre formation | ||||
| Fibronectin matrix formation | |||||
| Cell surface interactions at the vascular wall | |||||
| Integrin cell surface interactions | |||||
| WikiPathways | Focal Adhesion | ||||
| Extracellular matrix organization | |||||
| Elastic fibre formation | |||||
| Arrhythmogenic Right Ventricular Cardiomyopathy | |||||
| Integrin-mediated Cell Adhesion | |||||
| L1CAM interactions | |||||
| Integrin cell surface interactions | |||||
| Cell surface interactions at the vascular wall | |||||
| References | |||||
| Ref 522128 | ClinicalTrials.gov (NCT00536016) A Phase 1 Safety Study of Single and Repeated Doses of JSM6427 (Intravitreal Injection) to Treat AMD. U.S. National Institutes of Health. | ||||
| Ref 546708 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009742) | ||||
| Ref 547054 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012564) | ||||
| Ref 526326 | Eosinophil adhesion to cholinergic nerves via ICAM-1 and VCAM-1 and associated eosinophil degranulation. Am J Physiol Lung Cell Mol Physiol. 2002 Jun;282(6):L1279-88. | ||||
| Ref 529125 | J Med Chem. 2007 Nov 29;50(24):5878-81. Epub 2007 Nov 1.Multiple N-methylation by a designed approach enhances receptor selectivity. | ||||
| Ref 536198 | Suppression and regression of choroidal neovascularization by systemic administration of an alpha5beta1 integrin antagonist. Mol Pharmacol. 2006 Jun;69(6):1820-8. Epub 2006 Mar 9. | ||||
| Ref 536506 | Modulation of hypoxia-induced neovascularization by JSM6427, an integrin alpha5beta1 inhibiting molecule. Curr Eye Res. 2007 Sep;32(9):801-12. | ||||
| Ref 536855 | An alpha5beta1 integrin inhibitor attenuates glioma growth. Mol Cell Neurosci. 2008 Dec;39(4):579-85. Epub 2008 Sep 4. | ||||
| Ref 544129 | Roles of integrin activation in eosinophil function and the eosinophilic inflammation of asthma. J Leukoc Biol. 2008 January; 83(1): 1-12. | ||||
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