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Integrins C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Integrins are unusual signalling proteins that function to signal both from the extracellular environment into the cell, but also from the cytoplasm to the external of the cell. The intracellular signalling cascades associated with integrin activation focus on protein kinase activities, such as focal adhesion kinase and Src. Based on this association between extracellular signals and intracellular protein kinase activity, we have chosen to include integrins in the 'Catalytic receptors' section of the database until more stringent criteria from NC-IUPHAR allows precise definition of their classification.

Integrins are heterodimeric entities, composed of α and β subunits, each 1TM proteins, which bind components of the extracellular matrix or counter-receptors expressed on other cells. One class of integrin contains an inserted domain (I) in its α subunit, and if present (in α1, α2, α10, α11, αD, αE, αL, αM and αX), this I domain contains the ligand binding site. All β subunits possess a similar I-like domain, which has the capacity to bind ligand, often recognising the RGD motif. The presence of an α subunit I domain precludes ligand binding through the β subunit. Integrins provide a link between ligand and the actin cytoskeleton (through typically short intracellular domains). Integrins bind several divalent cations, including a Mg2+ ion in the I or I-like domain that is essential for ligand binding. Other cation binding sites may regulate integrin activity or stabilise the 3D structure. Integrins regulate the activity of particular protein kinases, including focal adhesion kinase and integrin-linked kinase. Cellular activation regulates integrin ligand affinity via inside-out signalling and ligand binding to integrins can regulate cellular activity via outside-in signalling.

Several drugs that target integrins are in clinical use including: (1) abciximab (αIIbβ3) for short term prevention of coronary thrombosis, (2) vedolizumab (α4β7) to reduce gastrointestinal inflammation, and (3) natalizumab (α4β1) in some cases of severe multiple sclerosis.

Receptors

2460
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Complexes

integrin α1β1 C Show summary »

integrin α2β1 C Show summary »

integrin αIIbβ3 C Show summary » More detailed page go icon to follow link

integrin α4β1 C Show summary » More detailed page go icon to follow link

integrin α4β7 C Show summary » More detailed page go icon to follow link

integrin α5β1 C Show summary »

integrin α6β1 C Show summary »

integrin α10β1 C Show summary »

integrin α11β1 C Show summary »

integrin αEβ7 C Show summary »

integrin αLβ2 C Show summary »

integrin αVβ3 C Show summary »

Receptors and Subunits

integrin, alpha 1 subunit C Show summary »

integrin, alpha 2 subunit (CD49B, alpha 2 subunit of VLA-2 receptor) C Show summary »

integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41) C Show summary »

integrin, alpha 3 subunit (antigen CD49C, alpha 3 subunit of VLA-3 receptor) C Show summary »

integrin, alpha 4 subunit (antigen CD49D, alpha 4 subunit of VLA-4 receptor) C Show summary » More detailed page go icon to follow link

integrin, alpha 5 subunit (fibronectin receptor, alpha polypeptide) C Show summary »

integrin, alpha 6 subunit C Show summary »

integrin, alpha 7 subunit C Show summary »

integrin, alpha 8 subunit C Show summary »

integrin, alpha 9 subunit C Show summary »

integrin, alpha 10 subunit C Show summary »

integrin, alpha 11 subunit C Show summary »

integrin, alpha D subunit C Show summary »

integrin, alpha E subunit (antigen CD103, human mucosal lymphocyte antigen 1; alpha polypeptide) C Show summary »

integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide) C Show summary » More detailed page go icon to follow link

integrin, alpha M subunit (complement component 3 receptor 3 subunit) C Show summary »

integrin, alpha V subunit C Show summary » More detailed page go icon to follow link

integrin, alpha X subunit (complement component 3 receptor 4 subunit) C Show summary »

integrin, beta 1 subunit (fibronectin receptor, beta polypeptide, antigen CD29 includes MDF2, MSK12) C Show summary » More detailed page go icon to follow link

integrin, beta 2 subunit (complement component 3 receptor 3 and 4 subunit) C Show summary » More detailed page go icon to follow link

integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61) C Show summary »

integrin, beta 4 subunit C Show summary »

integrin, beta 5 subunit C Show summary »

integrin, beta 6 subunit C Show summary »


Target Id 2460
Nomenclature integrin, beta 6 subunit
Previous and unofficial names integrin subunit beta 6 | integrin beta 6
Genes ITGB6 (Hs), Itgb6 (Mm), Itgb6 (Rn)
Ensembl ID ENSG00000115221 (Hs), ENSMUSG00000026971 (Mm), ENSRNOG00000008346 (Rn)
UniProtKB AC P18564 (Hs), Q9Z0T9 (Mm), Q6AYF4 (Rn)
Selective inhibitors
compound 7 [PMID: 31381331] pKi 10.0 [2]

integrin, beta 7 subunit C Show summary »

integrin, beta 8 subunit C Show summary »

Comments

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Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Catalytic receptors. Br J Pharmacol. 180 Suppl 2:S241-288.