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integrin α4β7

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Target not currently curated in GtoImmuPdb

Target id: 2770

Nomenclature: integrin α4β7

Family: Integrins

Contents:

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
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
etrolizumab Peptide Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Binding 10.1 pIC50 1
⤷ pIC50 10.1 (IC50 7.5x10-11 M) [1]
Description: Inhibition of β7-MAdCAM-1-mediated cell adhesion.
carotegrast Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 4
⤷ pIC50 8.5 (IC50 3.3x10-9 M) [4]
Description: Measuring inhibition of binding between &alpha4;β7 integrin expressed by RPMI-8866 cells and immobilised VCAM-1, in the presence of test compound.
firategrast Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition - - 2
⤷ [2]
valategrast Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition - - 3
⤷ [3]
zaurategrast Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition - - 7
⤷ [7]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
vedolizumab Peptide Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 8.3 pIC50 5
⤷ pIC50 8.3 (IC50 5.34x10-9 M) [5]
Description: Binding to HuT-78 cells
Antibody Comments
Vedolizumab binds to this integrin which is expressed on subsets of leucocytes [6].

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. Grove RA, Shackelford S, Sopper S, Pirruccello S, Horrigan J, Havrdova E, Gold M, Graff O. (2013) Leukocyte counts in cerebrospinal fluid and blood following firategrast treatment in subjects with relapsing forms of multiple sclerosis. Eur J Neurol, 20 (7): 1032-42. [PMID:23419064]

3. Hijazi Y, Welker H, Dorr AE, Tang JP, Blain R, Renzetti LM, Abbas R. (2004) Pharmacokinetics, safety, and tolerability of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist after oral administration at single and multiple once-daily ascending doses in healthy volunteers. J Clin Pharmacol, 44 (12): 1368-78. [PMID:15545307]

4. 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.

5. 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.

6. 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]

7. Wolf C, Sidhu J, Otoul C, Morris DL, Cnops J, Taubel J, Bennett B. (2013) Pharmacodynamic consequences of administration of VLA-4 antagonist CDP323 to multiple sclerosis subjects: a randomized, double-blind phase 1/2 study. PLoS One, 8 (3): e58438. [PMID:23472197]

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