Target General Infomation
Target ID
T55293
Former ID
TTDR00276
Target Name
Integrin alpha-2
Gene Name
ITGA2
Synonyms
Adhesive platelet receptor alpha1 beta2; Alpha 2 beta 1 integrin; CD49b; Collagen receptor; GPIa; GPIa/IIa; Glycoprotein Ia-IIa; Integrin alpha(2)beta(1); Integrin alpha2beta 1; Platelet glycoprotein Ia/IIa; Platelet membrane glycoprotein Ia; VLA-2; VLA-2 alphachain; ITGA2
Target Type
Clinical Trial
Disease Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Integrin alpha-2/beta-1 is a receptor for laminin, collagen, collagen C-propeptides, fibronectin and E-cadherin. It recognizes the proline-hydroxylated sequence G-F-P-G-E-R in collagen. It is responsible for adhesion of platelets and other cells to collagens, modulation of collagen and collagenase gene expression, force generation and organization of newly synthesized extracellular matrix.
BioChemical Class
Integrin
Target Validation
T55293
UniProt ID
Sequence
MGPERTGAAPLPLLLVLALSQGILNCCLAYNVGLPEAKIFSGPSSEQFGYAVQQFINPKG
NWLLVGSPWSGFPENRMGDVYKCPVDLSTATCEKLNLQTSTSIPNVTEMKTNMSLGLILT
RNMGTGGFLTCGPLWAQQCGNQYYTTGVCSDISPDFQLSASFSPATQPCPSLIDVVVVCD
ESNSIYPWDAVKNFLEKFVQGLDIGPTKTQVGLIQYANNPRVVFNLNTYKTKEEMIVATS
QTSQYGGDLTNTFGAIQYARKYAYSAASGGRRSATKVMVVVTDGESHDGSMLKAVIDQCN
HDNILRFGIAVLGYLNRNALDTKNLIKEIKAIASIPTERYFFNVSDEAALLEKAGTLGEQ
IFSIEGTVQGGDNFQMEMSQVGFSADYSSQNDILMLGAVGAFGWSGTIVQKTSHGHLIFP
KQAFDQILQDRNHSSYLGYSVAAISTGESTHFVAGAPRANYTGQIVLYSVNENGNITVIQ
AHRGDQIGSYFGSVLCSVDVDKDTITDVLLVGAPMYMSDLKKEEGRVYLFTIKKGILGQH
QFLEGPEGIENTRFGSAIAALSDINMDGFNDVIVGSPLENQNSGAVYIYNGHQGTIRTKY
SQKILGSDGAFRSHLQYFGRSLDGYGDLNGDSITDVSIGAFGQVVQLWSQSIADVAIEAS
FTPEKITLVNKNAQIILKLCFSAKFRPTKQNNQVAIVYNITLDADGFSSRVTSRGLFKEN
NERCLQKNMVVNQAQSCPEHIIYIQEPSDVVNSLDLRVDISLENPGTSPALEAYSETAKV
FSIPFHKDCGEDGLCISDLVLDVRQIPAAQEQPFIVSNQNKRLTFSVTLKNKRESAYNTG
IVVDFSENLFFASFSLPVDGTEVTCQVAASQKSVACDVGYPALKREQQVTFTINFDFNLQ
NLQNQASLSFQALSESQEENKADNLVNLKIPLLYDAEIHLTRSTNINFYEISSDGNVPSI
VHSFEDVGPKFIFSLKVTTGSVPVSMATVIIHIPQYTKEKNPLMYLTGVQTDKAGDISCN
ADINPLKIGQTSSSVSFKSENFRHTKELNCRTASCSNVTCWLKDVHMKGEYFVNVTTRIW
NGTFASSTFQTVQLTAAAEINTYNPEIYVIEDNTVTIPLMIMKPDEKAEVPTGVIIGSII
AGILLLLALVAILWKLGFFKRKYEKMTKNPDEIDETTELSS
Drugs and Mode of Action
Drug(s) E7820 Drug Info Phase 2 Solid tumours [531326]
Inhibitor 3-(3-(benzamido)-5-nitrobenzamido)propanoic acid Drug Info [528383]
3-(3-(carbamoyl)benzamido)-3-phenylpropanoic acid Drug Info [528383]
3-(3-(carbamoyl)benzamido)propanoic acid Drug Info [528383]
E7820 Drug Info [531326]
MAGGIEMYCIN Drug Info [528798]
Pathways
KEGG Pathway Phagosome
PI3K-Akt signaling pathway
Focal adhesion
ECM-receptor interaction
Platelet activation
Hematopoietic cell lineage
Regulation of actin cytoskeleton
Pathways in cancer
Proteoglycans in cancer
Small cell lung cancer
Hypertrophic cardiomyopathy (HCM)
Arrhythmogenic right ventricular cardiomyopathy (ARVC)
Dilated cardiomyopathy
NetPath Pathway IL4 Signaling Pathway
EGFR1 Signaling Pathway
PANTHER Pathway Integrin signalling pathway
Pathway Interaction Database Beta1 integrin cell surface interactions
Integrin family cell surface interactions
Arf6 trafficking events
CXCR4-mediated signaling events
Plexin-D1 Signaling
Syndecan-2-mediated signaling events
VEGFR3 signaling in lymphatic endothelium
Reactome Integrin cell surface interactions
Laminin interactions
Syndecan interactions
ECM proteoglycans
CHL1 interactions
Platelet Adhesion to exposed collagen
WikiPathways TGF beta Signaling Pathway
Focal Adhesion
Human Complement System
Extracellular matrix organization
Interleukin-11 Signaling Pathway
Arrhythmogenic Right Ventricular Cardiomyopathy
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
Platelet Adhesion to exposed collagen
Integrin-mediated Cell Adhesion
L1CAM interactions
Integrin cell surface interactions
References
Ref 531326Phase I study of E7820, an oral inhibitor of integrin alpha-2 expression with antiangiogenic properties, in patients with advanced malignancies. Clin Cancer Res. 2011 Jan 1;17(1):193-200.
Ref 528383Bioorg Med Chem Lett. 2006 Oct 15;16(20):5294-7. Epub 2006 Aug 21.Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists.
Ref 528798J Med Chem. 2007 May 31;50(11):2742-6. Epub 2007 Apr 21.Small molecule designed to target metal binding site in the alpha2I domain inhibits integrin function.
Ref 531326Phase I study of E7820, an oral inhibitor of integrin alpha-2 expression with antiangiogenic properties, in patients with advanced malignancies. Clin Cancer Res. 2011 Jan 1;17(1):193-200.

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