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integrin, alpha V subunit

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Target id: 2453

Nomenclature: integrin, alpha V subunit

Family: Integrins

Contents:

Quaternary Structure: Complexes
integrin αVβ3
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1048 2q32.1 ITGAV integrin subunit alpha V
Mouse 1 1044 2 49.33 cM Itgav integrin alpha V
Rat - - 3q24 Itgav integrin subunit alpha V
Previous and Unofficial Names Click here for help
VNRA | VTNR | CD51 | MSK8 | Vitronectin receptor subunit alpha
Database Links Click here for help
Alphafold P06756 (Hs), P43406 (Mm)
ChEMBL Target CHEMBL3660 (Hs), CHEMBL4523628 (Mm), CHEMBL3430891 (Mm)
DrugBank Target P06756 (Hs)
Ensembl Gene ENSG00000138448 (Hs), ENSMUSG00000027087 (Mm), ENSRNOG00000004912 (Rn)
Entrez Gene 3685 (Hs), 16410 (Mm), 296456 (Rn)
Human Protein Atlas ENSG00000138448 (Hs)
KEGG Gene hsa:3685 (Hs), mmu:16410 (Mm), rno:296456 (Rn)
OMIM 193210 (Hs)
Pharos P06756 (Hs)
RefSeq Nucleotide NM_001144999 (Hs), NM_002210 (Hs), NM_008402 (Mm)
RefSeq Protein NP_002201 (Hs), NP_001138471 (Hs), NP_032428 (Mm)
UniProtKB P06756 (Hs), P43406 (Mm)
Wikipedia ITGAV (Hs)

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Inhibitor Comments
Bexotegrast binds to αVβ6 with an IC50 of 5700 nM [1].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK3008348 Small molecule or natural product Hs Antagonist 10.8 pKd 2
⤷ pKd 10.8 (Kd 1.57x10-11 M) [2]
Description: Binding affinity of the tritiated radioligand for recpmbinant human αVβ6 integrin
MK-0429 Small molecule or natural product Hs Antagonist 7.1 pIC50 4
⤷ pIC50 7.1 (IC50 8x10-8 M) [4]
Description: Binding to the αvβ3 integrin using a scintillation-proximity assay (SPAV3).
bexotegrast Small molecule or natural product Hs Antagonist 5.5 pIC50 1
⤷ pIC50 5.5 (IC50 3.4x10-6 M) [1]
Description: Determined in a human αVβ1 ligand binding assay
Immuno Process Associations
Immuno Process:  Barrier integrity
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
Immuno Process:  Cytokine production & signalling
Immuno Process:  T cell (activation)
General Comments
The αv integrins (especially αvβ6) have been identified as playing a key role in the development of idiopathic pulmonary fibrosis (IPF) [3]. Pan αv inhibitors are therefore being examined for clinical utlility as treatments for IPF.

References

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1. Decaris ML, Schaub JR, Chen C, Cha J, Lee GG, Rexhepaj M, Ho SS, Rao V, Marlow MM, Kotak P et al.. (2021) Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF. Respir Res, 22 (1): 265. [PMID:34666752]

2. Hall ER, Bibby LI, Slack RJ. (2016) Characterisation of a novel, high affinity and selective αvβ6 integrin RGD-mimetic radioligand. Biochem Pharmacol, 117: 88-96. [PMID:27501918]

3. Henderson NC, Arnold TD, Katamura Y, Giacomini MM, Rodriguez JD, McCarty JH, Pellicoro A, Raschperger E, Betsholtz C, Ruminski PG et al.. (2013) Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs. Nat Med, 19 (12): 1617-24. [PMID:24216753]

4. Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD et al.. (2003) Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. J Med Chem, 46 (22): 4790-8. [PMID:14561098]

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