General Information of the Protein
Protein ID
PT03794
Protein Name
Integrin alpha-V
Secondarily
Protein Name
Vitronectin receptor
Vitronectin receptor subunit alpha
Gene Name
ITGAV
Secondarily
Gene Name
MSK8
VNRA
VTNR
Sequence
MAFPPRRRLRLGPRGLPLLLSGLLLPLCRAFNLDVDSPAEYSGPEGSYFGFAVDFFVPSASSRMFLLVGAPKANTTQPGIVEGGQVLKCDWSSTRRCQPIEFDATGNRDYAKDDPLEFKSHQWFGASVRSKQDKILACAPLYHWRTEMKQEREPVGTCFLQDGTKTVEYAPCRSQDIDADGQGFCQGGFSIDFTKADRVLLGGPGSFYWQGQLISDQVAEIVSKYDPNVYSIKYNNQLATRTAQAIFDDSYLGYSVAVGDFNGDGIDDFVSGVPRAARTLGMVYIYDGKNMSSLYNFTGEQMAAYFGFSVAATDINGDDYADVFIGAPLFMDRGSDGKLQEVGQVSVSLQRASGDFQTTKLNGFEVFARFGSAIAPLGDLDQDGFNDIAIAAPYGGEDKKGIVYIFNGRSTGLNAVPSQILEGQWAARSMPPSFGYSMKGATDIDKNGYPDLIVGAFGVDRAILYRARPVITVNAGLEVYPSILNQDNKTCSLPGTALKVSCFNVRFCLKADGKGVLPRKLNFQVELLLDKLKQKGAIRRALFLYSRSPSHSKNMTISRGGLMQCEELIAYLRDESEFRDKLTPITIFMEYRLDYRTAADTTGLQPILNQFTPANISRQAHILLDCGEDNVCKPKLEVSVDSDQKKIYIGDDNPLTLIVKAQNQGEGAYEAELIVSIPLQADFIGVVRNNEALARLSCAFKTENQTRQVVCDLGNPMKAGTQLLAGLRFSVHQQSEMDTSVKFDLQIQSSNLFDKVSPVVSHKVDLAVLAAVEIRGVSSPDHVFLPIPNWEHKENPETEEDVGPVVQHIYELRNNGPSSFSKAMLHLQWPYKYNNNTLLYILHYDIDGPMNCTSDMEINPLRIKISSLQTTEKNDTVAGQGERDHLITKRDLALSEGDIHTLGCGVAQCLKIVCQVGRLDRGKSAILYVKSLLWTETFMNKENQNHSYSLKSSASFNVIEFPYKNLPIEDITNSTLVTTNVTWGIQPAPMPVPVWVIILAVLAGLLLLAVLVFVMYRMGFFKRVRPPQEEQEREQLQPHENGEGNSET
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
Function
The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fibrinogen, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin and vWF. They recognize the sequence R-G-D in a wide array of ligands. ITGAV:ITGB3 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 and ITGAV:ITGB6 act as receptors for fibrillin-1 (FBN1) and mediate R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887, PubMed:17158881). Integrin alpha-V/beta-6 or alpha-V/beta-8 (ITGAV:ITGB6 or ITGAV:ITGB8) mediates R-G-D-dependent release of transforming growth factor beta-1 (TGF-beta-1) from regulatory Latency-associated peptide (LAP), thereby playing a key role in TGF-beta-1 activation (PubMed:15184403, PubMed:22278742, PubMed:28117447). ITGAV:ITGB3 acts as a receptor for CD40LG (PubMed:31331973).
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Uniprot ID
Primary ID:
P06756

Secondarily ID:
A0AV67
B0LPF4
B7Z883
B7ZLX0
D3DPG8
E7EWZ6
Q53SK4
Q59EB7
Q6LD15
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Ensembl ID
ENSG00000138448
HGNC ID
HGNC:6150
Subcellular Location
Cell membrane
Cell junction
Focal adhesion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000048 , PC-3
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0636915
 Compound Info 
2-[(2S,5R,8S,11S)-5-benzyl-11-(3-carbamimidamidopropyl)-8-({4-[(2-{2-[2-({N'-[(1E)-[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]methylidene]hydrazinecarbonyl}methoxy)ethoxy]ethoxy}acetamido)methyl]phenyl}methyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid
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C60H69N13O16
  1
1
IC50 = 4800 nM
 Bioactivity Info 
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CP0000897
 Compound Info 
2-[(2S,5R,8S,11S)-5-benzyl-11-(3-carbamimidamidopropyl)-8-{3-[(2-{[(Z)-{[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]methylidene}amino]oxy}ethyl)carbamoyl]propyl}-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid
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C50H58N12O13
  1
1
IC50 = 5800 nM
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CP0004991
 Compound Info 
2-[(2S,5R,8S,11S)-5-benzyl-11-(3-carbamimidamidopropyl)-8-{[4-({2-[2-(2-{[(2-{[(E)-{[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]methylidene}amino]oxy}ethyl)carbamoyl]methoxy}ethoxy)ethoxy]acetamido}methyl)phenyl]methyl}-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid
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C62H73N13O17
  1
1
IC50 = 8300 nM
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CP0637030
 Compound Info 
2-[(2S,5R,8S,11S)-5-benzyl-11-(3-carbamimidamidopropyl)-8-({4-[(2-{2-[2-({N'-[(1E)-3-[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]propylidene]hydrazinecarbonyl}methoxy)ethoxy]ethoxy}acetamido)methyl]phenyl}methyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid
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C62H73N13O16
  1
1
IC50 = 11000 nM
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CP0011035
 Compound Info 
2-((2S,5R,8S,11S)-5-benzyl-11-(3-guanidinopropyl)-8-(4-(13-hydrazinyl-3,13-dioxo-5,8,11-trioxa-2-azatridecyl)phenyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)acetic acid
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C38H53N11O12
  1
1
IC50 = 15600 nM
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CP0633534
 Compound Info 
1-(4-((5S,11S,14R)-14-benzyl-11-(carboxymethyl)-5-(3-guanidinopropyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)phenyl)-3-oxo-5,8,11-trioxa-2-azatridecan-13-oic acid
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C38H51N9O13
  1
1
IC50 = 18800 nM
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CP0004329
 Compound Info 
4-(4-((2S,5S,11S,14R)-14-benzyl-11-(carboxymethyl)-5-(3-guanidinopropyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)benzylamino)-4-oxobutanoic acid
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C34H43N9O10
  1
1
IC50 = 33700 nM
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CP0004249
 Compound Info 
4-((2S,5S,11S,14R)-14-benzyl-11-(carboxymethyl)-5-(3-guanidinopropyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)butanoic acid
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C27H38N8O9
  1
1
IC50 = 38800 nM
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CP0001576
 Compound Info 
2-[(2S,5R,8S,11S)-5-benzyl-11-(3-carbamimidamidopropyl)-8-{[4-({3-[(2-{[(E)-{[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]methylidene}amino]oxy}ethyl)carbamoyl]propanamido}methyl)phenyl]methyl}-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid
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C58H65N13O14
  1
1
IC50 > 100000 nM
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Clinical Information about the Protein
Target 1 ( Integrin alpha-V (ITGAV) )
Target Type Clinical trial Target
Target 2 ( ITGAV messenger RNA (ITGAV mRNA) )
Target Type Clinical trial Target