Target General Infomation
Target ID
T67363
Former ID
TTDI01789
Target Name
Integrin alpha-5/beta-3
Gene Name
ITGB3
Synonyms
ITGB3
Target Type
Clinical Trial
Disease Renal cancer [ICD9: 140-229, 189; ICD10: C64]
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.
BioChemical Class
Integrin
UniProt ID
Sequence
MRARPRPRPLWATVLALGALAGVGVGGPNICTTRGVSSCQQCLAVSPMCAWCSDEALPLG
SPRCDLKENLLKDNCAPESIEFPVSEARVLEDRPLSDKGSGDSSQVTQVSPQRIALRLRP
DDSKNFSIQVRQVEDYPVDIYYLMDLSYSMKDDLWSIQNLGTKLATQMRKLTSNLRIGFG
AFVDKPVSPYMYISPPEALENPCYDMKTTCLPMFGYKHVLTLTDQVTRFNEEVKKQSVSR
NRDAPEGGFDAIMQATVCDEKIGWRNDASHLLVFTTDAKTHIALDGRLAGIVQPNDGQCH
VGSDNHYSASTTMDYPSLGLMTEKLSQKNINLIFAVTENVVNLYQNYSELIPGTTVGVLS
MDSSNVLQLIVDAYGKIRSKVELEVRDLPEELSLSFNATCLNNEVIPGLKSCMGLKIGDT
VSFSIEAKVRGCPQEKEKSFTIKPVGFKDSLIVQVTFDCDCACQAQAEPNSHRCNNGNGT
FECGVCRCGPGWLGSQCECSEEDYRPSQQDECSPREGQPVCSQRGECLCGQCVCHSSDFG
KITGKYCECDDFSCVRYKGEMCSGHGQCSCGDCLCDSDWTGYYCNCTTRTDTCMSSNGLL
CSGRGKCECGSCVCIQPGSYGDTCEKCPTCPDACTFKKECVECKKFDRGALHDENTCNRY
CRDEIESVKELKDTGKDAVNCTYKNEDDCVVRFQYYEDSSGKSILYVVEEPECPKGPDIL
VVLLSVMGAILLIGLAALLIWKLLITIHDRKEFAKFEEERARAKWDTANNPLYKEATSTF
TNITYRGT
Structure
3VI3; 3VI4; 4WJK; 4WK0; 4WK2; 4WK4
Drugs and Mode of Action
Drug(s) ATN-161 Drug Info Phase 2 Renal cancer [521662]
Antagonist ATN-161 Drug Info [528439]
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
Reactome Platelet degranulation
Elastic fibre formation
Fibronectin matrix formation
PECAM1 interactions
Molecules associated with elastic fibres
Integrin cell surface interactions
Syndecan interactions
ECM proteoglycans
Integrin alphaIIb beta3 signaling
SOS provides linkage to MAPK signaling for Integrins
p130Cas linkage to MAPK signaling for integrins
VEGFA-VEGFR2 Pathway
MAP2K and MAPK activation
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 521662ClinicalTrials.gov (NCT00131651) ATN-161 in Advanced Renal Cell Cancer. U.S. National Institutes of Health.
Ref 528439A non-RGD-based integrin binding peptide (ATN-161) blocks breast cancer growth and metastasis in vivo. Mol Cancer Ther. 2006 Sep;5(9):2271-80.

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