Quaternary Structure: Complexes

integrin αVβ3

Gene and Protein Information
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

CD51 | MSK8 | Vitronectin receptor subunit alpha | VNRA | VTNR

Database Links
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 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 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 Hs Antagonist 5.5 pIC50 1 ⤷ pIC50 5.5 (IC50 3.4x10-6 M) [1] Description: Determined in a human αVβ1 ligand binding assay

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.