integrin α4β1 | Integrins | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

integrin α4β1

Target not currently curated in GtoImmuPdb

Target id: 2580

Nomenclature: integrin α4β1

Family: Integrins

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Quaternary Structure: Subunits
integrin, alpha 4 subunit (antigen CD49D, alpha 4 subunit of VLA-4 receptor)
integrin, beta 1 subunit (fibronectin receptor, beta polypeptide, antigen CD29 includes MDF2, MSK12)
Previous and Unofficial Names
very late antigen-4 | VLA-4
Ligands (Human)
fibronectin (FN1, P02751), vascular cell adhesion protein 1 (VCAM1, P19320), osteopontin (SPP1, P10451), thrombospondin

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BIO1211 Hs Inhibition 8.3 – 9.0 pIC50 1
pIC50 8.3 – 9.0 [1]
TCS2314 Hs Inhibition - -
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
carotegrast Hs Antagonist 7.2 pIC50 2
pIC50 7.2 (IC50 5.7x10-8 M) [2]
Description: Measuring inhibition of binding between &alpha4;β1 integrin expressed by Jurkat cells and immobilised VCAM-1, in the presence of test compound.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
natalizumab Hs Inhibition - - 3
[3]
Antibody Comments
Approved antibody drug natalizumab has the integrin α4 subunit as its primary target.

References

Show »

1. Lin Kc, Ateeq HS, Hsiung SH, Chong LT, Zimmerman CN, Castro A, Lee WC, Hammond CE, Kalkunte S, Chen LL et al.. (1999) Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses. J. Med. Chem., 42 (5): 920-34. [PMID:10072689]

2. Makino S, Okuzumi T, Yoshimura T, Satake Y, Suzuki N, Izawa H, Sagi K, Chiba A, Nakanishi E, Murata M et al.. (2011) New phenylalanine derivatives. Patent number: US20110065918A1. Assignee: EA Pharma Co Ltd. Priority date: 18/08/2000. Publication date: 17/03/2011.

3. No authors listed. (2004) Natalizumab: AN 100226, anti-4alpha integrin monoclonal antibody. Drugs R D, 5 (2): 102-7. [PMID:15293871]

How to cite this page

Select citation format: