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integrin, alpha V subunit

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Target not currently curated in GtoImmuPdb

Target id: 2453

Nomenclature: integrin, alpha V subunit

Family: Integrins

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
VTNR | CD51 | MSK8 | Vitronectin receptor subunit alpha | VNRA
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein

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Inhibitor Comments
Bexotegrast binds to αVβ6 with an IC50 of 5700 nM [1].
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.


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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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