integrin α4β7 | Integrins | IUPHAR/BPS Guide to PHARMACOLOGY

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integrin α4β7

Target not currently curated in GtoImmuPdb

Target id: 2770

Nomenclature: integrin α4β7

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 7 subunit

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Inhibitors
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Ligand Sp. Action Value Parameter Reference
etrolizumab Hs Binding 10.1 pIC50 1
pIC50 10.1 (IC50 7.5x10-11 M) [1]
Description: Inhibition of β7-MAdCAM-1-mediated cell adhesion.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
carotegrast Hs Antagonist 8.5 pIC50 2
pIC50 8.5 (IC50 3.3x10-9 M) [2]
Description: Measuring inhibition of binding between &alpha4;β7 integrin expressed by RPMI-8866 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
vedolizumab Hs Antagonist 8.3 pIC50 3
pIC50 8.3 (IC50 5.34x10-9 M) [3]
Description: Binding to HuT-78 cells
Antibody Comments
Vedolizumab binds to this integrin which is expressed on subsets of leucocytes [4].

References

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1. Fong S, Dennis MS. (2009) Humanized anti-beta7 antagonists and uses therefor. Patent number: US7528236 B2. Assignee: Genentech, Inc.. Priority date: 03/09/2004. Publication date: 09/05/2009.

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. Ponath PD, Ringler DJ, ST, Newman W, Saldanha J, Bendig MM. (2006) Humanized immunoglobulin reactive with α4β7 integrin. Patent number: US7147851 B1. Assignee: Millennium Pharmaceuticals, Inc.. Priority date: 15/08/1996. Publication date: 12/12/2006.

4. Soler D, Chapman T, Yang LL, Wyant T, Egan R, Fedyk ER. (2009) The binding specificity and selective antagonism of vedolizumab, an anti-alpha4beta7 integrin therapeutic antibody in development for inflammatory bowel diseases. J. Pharmacol. Exp. Ther., 330 (3): 864-75. [PMID:19509315]

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