Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T86130
|
||||
Former ID |
TTDI01797
|
||||
Target Name |
Integrin alpha-4/beta-1
|
||||
Target Type |
Clinical Trial
|
||||
Disease | Arthritis [ICD9: 710-719; ICD10: M00-M25] | ||||
Asthma [ICD10: J45] | |||||
Crohn's disease [ICD9: 555; ICD10: K50] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51] | |||||
Multiple scierosis [ICD9: 340; ICD10: G35] | |||||
Multiple sclerosis; Rheumatoid arthritis [ICD9: 340, 710-719, 714; ICD10: G35, M00-M25, M05-M06] | |||||
Relapsing forms of multiple sclerosis [ICD9: 340; ICD10: G35] | |||||
Function |
Integrins alpha-4/beta-1 (VLA-4) and alpha-4/beta-7 are receptors for fibronectin. They recognize one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. They are also receptors for VCAM1. Integrin alpha- 4/beta-1 recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha- 4/beta-7 is also a receptor for MADCAM1. It recognizes the sequence L-D-T in MADCAM1. On activated endothelial cells integrin VLA-4 triggers homotypic aggregation for most VLA-4-positive leukocyte cell lines. It may also participate in cytolytic T-cell interactions with target cells.
|
||||
BioChemical Class |
Integrin
|
||||
UniProt ID | |||||
Drugs and Mode of Action | |||||
Drug(s) | AJM-300 | Drug Info | Phase 3 | Crohn's disease | [547815] |
CDP323 | Drug Info | Phase 2 | Multiple sclerosis; Rheumatoid arthritis | [536651] | |
Firategrast | Drug Info | Phase 2 | Relapsing forms of multiple sclerosis | [547712] | |
R411 | Drug Info | Phase 2 | Asthma | [531186] | |
TRK-170 | Drug Info | Phase 2 | Inflammatory bowel disease | [523458] | |
HMR-1031 | Drug Info | Phase 1 | Arthritis | [526984] | |
TR-14035 | Drug Info | Discontinued in Phase 1 | Multiple scierosis | [547053] | |
CY-9652 | Drug Info | Terminated | Inflammatory disease | [546159] | |
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | PI3K-Akt signaling pathway | ||||
Focal adhesion | |||||
ECM-receptor interaction | |||||
Cell adhesion molecules (CAMs) | |||||
Hematopoietic cell lineage | |||||
Leukocyte transendothelial migration | |||||
Intestinal immune network for IgA production | |||||
Regulation of actin cytoskeleton | |||||
Leishmaniasis | |||||
Hypertrophic cardiomyopathy (HCM) | |||||
Arrhythmogenic right ventricular cardiomyopathy (ARVC) | |||||
Dilated cardiomyopathy | |||||
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 | |||||
WikiPathways | Focal Adhesion | ||||
Arrhythmogenic Right Ventricular Cardiomyopathy | |||||
Integrin-mediated Cell Adhesion | |||||
Integrin cell surface interactions | |||||
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell | |||||
Cell surface interactions at the vascular wall | |||||
References | |||||
Ref 523458 | ClinicalTrials.gov (NCT01345799) A Study of TRK-170 for the Treatment of Crohn's Disease. U.S. National Institutes of Health. | ||||
Ref 526984 | Pharmacoscintigraphic comparison of HMR 1031, a VLA-4 antagonist, in healthy volunteers following delivery via a nebulizer and a dry powder inhaler. Am J Ther. 2004 Mar-Apr;11(2):103-13. | ||||
Ref 531186 | Integrins as therapeutic targets: lessons and opportunities. Nat Rev Drug Discov. 2010 Oct;9(10):804-20. | ||||
Ref 546159 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006649) | ||||
Ref 547053 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012563) | ||||
Ref 526984 | Pharmacoscintigraphic comparison of HMR 1031, a VLA-4 antagonist, in healthy volunteers following delivery via a nebulizer and a dry powder inhaler. Am J Ther. 2004 Mar-Apr;11(2):103-13. | ||||
Ref 531186 | Integrins as therapeutic targets: lessons and opportunities. Nat Rev Drug Discov. 2010 Oct;9(10):804-20. | ||||
Ref 532326 | Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice. J Crohns Colitis. 2013 Dec;7(11):e533-42. | ||||
Ref 543650 | (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: 2580). |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.