Target Information

Target General Infomation
Target ID
T97353
Former ID
TTDI01786
Target Name
Integrin alpha-2/beta-1
Gene Name
ITGB1
Synonyms
ITGB1
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Multile sclerosis [ICD10: G35]
Multiple scierosis [ICD9: 340; ICD10: G35]
Function
Integrin alpha-2/beta-1 isa 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
UniProt ID
P05556
Sequence
MNLQPIFWIGLISSVCCVFAQTDENRCLKANAKSCGECIQAGPNCGWCTNSTFLQEGMPT
SARCDDLEALKKKGCPPDDIENPRGSKDIKKNKNVTNRSKGTAEKLKPEDITQIQPQQLV
LRLRSGEPQTFTLKFKRAEDYPIDLYYLMDLSYSMKDDLENVKSLGTDLMNEMRRITSDF
RIGFGSFVEKTVMPYISTTPAKLRNPCTSEQNCTSPFSYKNVLSLTNKGEVFNELVGKQR
ISGNLDSPEGGFDAIMQVAVCGSLIGWRNVTRLLVFSTDAGFHFAGDGKLGGIVLPNDGQ
CHLENNMYTMSHYYDYPSIAHLVQKLSENNIQTIFAVTEEFQPVYKELKNLIPKSAVGTL
SANSSNVIQLIIDAYNSLSSEVILENGKLSEGVTISYKSYCKNGVNGTGENGRKCSNISI
GDEVQFEISITSNKCPKKDSDSFKIRPLGFTEEVEVILQYICECECQSEGIPESPKCHEG
NGTFECGACRCNEGRVGRHCECSTDEVNSEDMDAYCRKENSSEICSNNGECVCGQCVCRK
RDNTNEIYSGKFCECDNFNCDRSNGLICGGNGVCKCRVCECNPNYTGSACDCSLDTSTCE
ASNGQICNGRGICECGVCKCTDPKFQGQTCEMCQTCLGVCAEHKECVQCRAFNKGEKKDT
CTQECSYFNITKVESRDKLPQPVQPDPVSHCKEKDVDDCWFYFTYSVNGNNEVMVHVVEN
PECPTGPDIIPIVAGVVAGIVLIGLALLLIWKLLMIIHDRREFAKFEKEKMNAKWDTGEN
PIYKSAVTTVVNPKYEGK
Structure
1AOX; 1DZI; 1PQB; 1V7P; 4BJ3
Drugs and Mode of Action
Drug(s) SAR-339658 Drug Info Phase 2 Inflammatory bowel disease [524009]
Valetizumab Drug Info Phase 2 Multile sclerosis [548114]
Vatelizumab Drug Info Phase 2 Multiple scierosis [524887]
Modulator Evatak Drug Info [543649]
Inhibitor TCI15 Drug Info [529918]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome Elastic fibre formation
Fibronectin matrix formation
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
Cell surface interactions at the vascular wall
Basigin interactions
Molecules associated with elastic fibres
Integrin cell surface interactions
Laminin interactions
Syndecan interactions
ECM proteoglycans
Other semaphorin interactions
Localization of the PINCH-ILK-PARVIN complex to focal adhesions
CHL1 interactions
RHO GTPases Activate Formins
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 524009ClinicalTrials.gov (NCT01659138) Efficacy and Safety of SAR339658 in Patients With Moderate to Severe Ulcerative Colitis. U.S. National Institutes of Health.
Ref 524887ClinicalTrials.gov (NCT02222948) Efficacy and Safety of Vatelizumab in Patients With Relapsing-Remitting Multiple Sclerosis. U.S. National Institutes of Health.
Ref 548114Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022066)
Ref 529918Small-molecule inhibitors of integrin alpha2beta1 that prevent pathological thrombus formation via an allosteric mechanism. Proc Natl Acad Sci U S A. 2009 Jan 20;106(3):719-24.
Ref 543649(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2578).
Ref 544483Sulfonamide inhibitors of alpha2beta1 integrin reveal the essential role of collagen receptors in in vivo models of inflammation. Pharmacol Res Perspect. 2015 June; 3(3): e00146.

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