integrin, alpha V subunit | Integrins | IUPHAR/BPS Guide to PHARMACOLOGY

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integrin, alpha V subunit

Target not currently curated in GtoImmuPdb

Target id: 2453

Nomenclature: integrin, alpha V subunit

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: Complexes
integrin αVβ3
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1048 2q31-q32 ITGAV integrin subunit alpha V
Mouse - 1044 2 D Itgav integrin alpha V
Rat - - 3q24 Itgav integrin subunit alpha V
Previous and Unofficial Names
CD51 | MSK8 | Vitronectin receptor subunit alpha | VNRA | VTNR
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
MK-0429 Hs Antagonist 7.1 pIC50 2
pIC50 7.1 (IC50 8x10-8 M) [2]
Description: Binding to the αvβ3 integrin using a scintillation-proximity assay (SPAV3).
Immuno Process Associations
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 4 GO processes
GO:0046718 viral entry into host cell IMP
GO:0052066 entry of symbiont into host cell by promotion of host phagocytosis NAS
GO:2000536 negative regulation of entry of bacterium into host cell IDA
click arrow to show/hide IEA associations
GO:0001618 virus receptor activity IEA
Immuno Process:  Inflammation
GO Annotations:  Associated to 6 GO processes
GO:0006954 inflammatory response TAS
GO:0043277 apoptotic cell clearance IGI
GO:0043312 neutrophil degranulation TAS
GO:0050764 regulation of phagocytosis IDA
GO:0050900 leukocyte migration TAS
GO:0052066 entry of symbiont into host cell by promotion of host phagocytosis NAS
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0002479 antigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependent TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0050900 leukocyte migration TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0042110 T cell activation TAS
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes, IEA only
GO:1901388 regulation of transforming growth factor beta activation IDA
click arrow to show/hide IEA associations
GO:0038044 transforming growth factor-beta secretion IEA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0042110 T cell activation TAS
General Comments
The αv integrins (especially αvβ6) have been identified as playing a key role in the development of idiopathic pulmonary fibrosis (IPF) [1]. Pan αv inhibitors are therefore being examined for clinical utlility as treatments for IPF.

References

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1. 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]

2. 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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