Target Information
Target General Infomation | |||||
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Target ID |
T67103
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Former ID |
TTDR00473
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Target Name |
Integrin alpha-V
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Gene Name |
ITGAV
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Synonyms |
CD51 antigen; Vitronectin receptor alpha subunit; ITGAV
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Target Type |
Clinical Trial
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Disease | Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | ||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
The alpha-v integrins are receptors for vitronectin, cytotactin, fibronectin, fibrinogen, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin and von willebrand factor. They recognize the sequence r-g-d.
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BioChemical Class |
Integrin
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Target Validation |
T67103
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UniProt ID | |||||
Sequence |
MAFPPRRRLRLGPRGLPLLLSGLLLPLCRAFNLDVDSPAEYSGPEGSYFGFAVDFFVPSA
SSRMFLLVGAPKANTTQPGIVEGGQVLKCDWSSTRRCQPIEFDATGNRDYAKDDPLEFKS HQWFGASVRSKQDKILACAPLYHWRTEMKQEREPVGTCFLQDGTKTVEYAPCRSQDIDAD GQGFCQGGFSIDFTKADRVLLGGPGSFYWQGQLISDQVAEIVSKYDPNVYSIKYNNQLAT RTAQAIFDDSYLGYSVAVGDFNGDGIDDFVSGVPRAARTLGMVYIYDGKNMSSLYNFTGE QMAAYFGFSVAATDINGDDYADVFIGAPLFMDRGSDGKLQEVGQVSVSLQRASGDFQTTK LNGFEVFARFGSAIAPLGDLDQDGFNDIAIAAPYGGEDKKGIVYIFNGRSTGLNAVPSQI LEGQWAARSMPPSFGYSMKGATDIDKNGYPDLIVGAFGVDRAILYRARPVITVNAGLEVY PSILNQDNKTCSLPGTALKVSCFNVRFCLKADGKGVLPRKLNFQVELLLDKLKQKGAIRR ALFLYSRSPSHSKNMTISRGGLMQCEELIAYLRDESEFRDKLTPITIFMEYRLDYRTAAD TTGLQPILNQFTPANISRQAHILLDCGEDNVCKPKLEVSVDSDQKKIYIGDDNPLTLIVK AQNQGEGAYEAELIVSIPLQADFIGVVRNNEALARLSCAFKTENQTRQVVCDLGNPMKAG TQLLAGLRFSVHQQSEMDTSVKFDLQIQSSNLFDKVSPVVSHKVDLAVLAAVEIRGVSSP DHVFLPIPNWEHKENPETEEDVGPVVQHIYELRNNGPSSFSKAMLHLQWPYKYNNNTLLY ILHYDIDGPMNCTSDMEINPLRIKISSLQTTEKNDTVAGQGERDHLITKRDLALSEGDIH TLGCGVAQCLKIVCQVGRLDRGKSAILYVKSLLWTETFMNKENQNHSYSLKSSASFNVIE FPYKNLPIEDITNSTLVTTNVTWGIQPAPMPVPVWVIILAVLAGLLLLAVLVFVMYRMGF FKRVRPPQEEQEREQLQPHENGEGNSET |
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Drugs and Mode of Action | |||||
Inhibitor | Ac-Asp-Arg-Leu-Asp-Ser-OH | Drug Info | [529045] | ||
AcDRGDS | Drug Info | [528659] | |||
C(-GRGDfL-) | Drug Info | [529125] | |||
C(Arg-Gly-Asp-D-Phe-Val) | Drug Info | [528215] | |||
C(RGDfF) | Drug Info | [528059] | |||
C(RGDfMeF) | Drug Info | [528059] | |||
C(RGDfV) | Drug Info | [528438] | |||
C-[-Arg-Gly-Asp-Acpca30-] | Drug Info | [527884] | |||
C-[-Arg-Gly-Asp-Acpca31-] | Drug Info | [527884] | |||
C-[-Arg-Gly-Asp-Acpca32-] | Drug Info | [527884] | |||
C-[-Arg-Gly-Asp-Acpca33-] | Drug Info | [527884] | |||
Cyclo(RGDfV) (control) | Drug Info | [528111] | |||
Cyclo-[-Arg-Gly-Asp-Amp21-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp22-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp23-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp24-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp25-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp26-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp27-] | Drug Info | [529343] | |||
Cyclo-[-Arg-Gly-Asp-Amp28-] | Drug Info | [529343] | |||
CYCLORGDFV | Drug Info | [530622] | |||
Cyclo[RGDfK(cypate)] | Drug Info | [528111] | |||
Cypate-[(RGD)2-NH2]1 | Drug Info | [528111] | |||
Cypate-[(RGD)2-NH2]2 | Drug Info | [528111] | |||
Cypate-[(RGD)3-NH2]1 | Drug Info | [528111] | |||
Cypate-[(RGD)3-NH2]2 | Drug Info | [528111] | |||
Cypate-[(RGD)4-NH2]1 | Drug Info | [528111] | |||
Cypate-[(RGD)4-NH2]2 | Drug Info | [528111] | |||
C[-Arg-Gly-Asp-Acpca19-] | Drug Info | [527884] | |||
C[-Arg-Gly-Asp-Acpca20-] | Drug Info | [527884] | |||
C[-Arg-Gly-Asp-Acpca21-] | Drug Info | [527884] | |||
C[-Arg-Gly-Asp-Acpca22-] | Drug Info | [527884] | |||
C[-Arg-Gly-Asp-Acpca34-] | Drug Info | [527884] | |||
C[-Arg-Gly-Asp-Acpca35-] | Drug Info | [527884] | |||
C[-Arg-Gly-Asp-Acpca36-] | Drug Info | [527884] | |||
C[RGD-(R)-alpha-TfmfV] | Drug Info | [528059] | |||
C[RGD-(S)-alpha-TfmfV] | Drug Info | [528059] | |||
C[RGDf-(3R)-Carboxymorpholine] | Drug Info | [529951] | |||
C[RGDf-(3S)-Carboxymorpholine] | Drug Info | [529951] | |||
C[RGDf-(R)-alpha-TfmF] | Drug Info | [528059] | |||
C[RGDf-(R)-alpha-TfmV] | Drug Info | [528059] | |||
C[RGDf-(R)-N-Me-alpha-TfmF] | Drug Info | [528059] | |||
C[RGDf-(S)-alpha-TfmF] | Drug Info | [528059] | |||
C[RGDf-(S)-alpha-TfmV] | Drug Info | [528059] | |||
C[RGDf-(S)-N-Me-alpha-TfmF] | Drug Info | [528059] | |||
C[RGDf-(S,R)-alpha-Dfm-F] | Drug Info | [528059] | |||
E[c(RGDyK)]2 | Drug Info | [527440] | |||
E[c(RGDyK)]2-PTX conjugate | Drug Info | [527440] | |||
G(D-Pen)-G-H-R-G-D-L-R-C-A | Drug Info | [533606] | |||
Gly-Arg-Gly-Asp-Ser | Drug Info | [530479] | |||
Gly-Arg-Gly-Asp-Ser-Pro-Lys | Drug Info | [525558] | |||
ISONIPECOTAMIDE | Drug Info | [527223] | |||
N-(3,5-dichlorophenyl)imidodicarbonimidic diamide | Drug Info | [530779] | |||
NAVPNLRGDLQVLAQKVART | Drug Info | [528633] | |||
RGDechi | Drug Info | [528215] | |||
SB-223245 | Drug Info | [534805] | |||
SB-265123 | Drug Info | [527268] | |||
ST-1646 | Drug Info | [529343] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Phagosome | ||||
PI3K-Akt signaling pathway | |||||
Focal adhesion | |||||
ECM-receptor interaction | |||||
Cell adhesion molecules (CAMs) | |||||
Regulation of actin cytoskeleton | |||||
Thyroid hormone signaling pathway | |||||
Pathways in cancer | |||||
Proteoglycans in cancer | |||||
Small cell lung cancer | |||||
Hypertrophic cardiomyopathy (HCM) | |||||
Arrhythmogenic right ventricular cardiomyopathy (ARVC) | |||||
Dilated cardiomyopathy | |||||
PANTHER Pathway | Integrin signalling pathway | ||||
CCKR signaling map ST | |||||
Pathway Interaction Database | Beta1 integrin cell surface interactions | ||||
Integrin family cell surface interactions | |||||
Beta3 integrin cell surface interactions | |||||
S1P3 pathway | |||||
Osteopontin-mediated events | |||||
Arf6 trafficking events | |||||
Nectin adhesion pathway | |||||
S1P1 pathway | |||||
CXCR4-mediated signaling events | |||||
Plexin-D1 Signaling | |||||
Integrins in angiogenesis | |||||
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
PDGFR-beta signaling pathway | |||||
PDGFR-alpha signaling pathway | |||||
Beta5 beta6 beta7 and beta8 integrin cell surface interactions | |||||
Signaling events mediated by VEGFR1 and VEGFR2 | |||||
Signaling events mediated by focal adhesion kinase | |||||
Reactome | Cross-presentation of particulate exogenous antigens (phagosomes) | ||||
Elastic fibre formation | |||||
PECAM1 interactions | |||||
Molecules associated with elastic fibres | |||||
Integrin cell surface interactions | |||||
Laminin interactions | |||||
Syndecan interactions | |||||
ECM proteoglycans | |||||
VEGFA-VEGFR2 Pathway | |||||
WikiPathways | Osteoblast Signaling | ||||
Focal Adhesion | |||||
Class I MHC mediated antigen processing & | |||||
presentation | |||||
Syndecan interactions | |||||
Extracellular matrix organization | |||||
Elastic fibre formation | |||||
Primary Focal Segmental Glomerulosclerosis FSGS | |||||
Arrhythmogenic Right Ventricular Cardiomyopathy | |||||
Integrin-mediated Cell Adhesion | |||||
L1CAM interactions | |||||
Integrin cell surface interactions | |||||
Cell surface interactions at the vascular wall | |||||
Osteopontin Signaling | |||||
References | |||||
Ref 522384 | ClinicalTrials.gov (NCT00721669) A Phase I Dose-Escalation Study of IMGN388 in Patients With Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 525558 | J Med Chem. 1999 Aug 12;42(16):3033-40.N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists. | ||||
Ref 527223 | Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins. | ||||
Ref 527268 | Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability. | ||||
Ref 527440 | J Med Chem. 2005 Feb 24;48(4):1098-106.Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery. | ||||
Ref 527884 | J Med Chem. 2005 Dec 1;48(24):7675-87.Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders. | ||||
Ref 528059 | J Med Chem. 2006 Mar 9;49(5):1808-17.Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior. | ||||
Ref 528111 | J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors. | ||||
Ref 528215 | J Med Chem. 2006 Jun 1;49(11):3416-20.Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior. | ||||
Ref 528438 | Bioorg Med Chem Lett. 2006 Nov 15;16(22):5878-82. Epub 2006 Sep 18.Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening. | ||||
Ref 528633 | J Biol Chem. 2007 Mar 30;282(13):9657-65. Epub 2007 Jan 23.Structure-function analysis of Arg-Gly-Asp helix motifs in alpha v beta 6 integrin ligands. | ||||
Ref 528659 | Bioorg Med Chem Lett. 2007 Apr 15;17(8):2329-33. Epub 2007 Jan 27.Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics. | ||||
Ref 529045 | Bioorg Med Chem. 2007 Dec 1;15(23):7380-90. Epub 2007 Aug 22.Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds. | ||||
Ref 529125 | J Med Chem. 2007 Nov 29;50(24):5878-81. Epub 2007 Nov 1.Multiple N-methylation by a designed approach enhances receptor selectivity. | ||||
Ref 529343 | J Med Chem. 2008 Mar 27;51(6):1771-82. Epub 2008 Feb 28.Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. | ||||
Ref 529951 | Bioorg Med Chem. 2009 Feb 15;17(4):1542-9. Epub 2009 Jan 13.Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity. | ||||
Ref 530479 | J Med Chem. 2009 Nov 26;52(22):7029-43.alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers. | ||||
Ref 530622 | J Med Chem. 2010 Jan 14;53(1):106-18.Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics. | ||||
Ref 530779 | J Med Chem. 2010 Jun 10;53(11):4332-53.Emerging targets in osteoporosis disease modification. | ||||
Ref 531160 | Anti-alphav integrin monoclonal antibody intetumumab enhances the efficacy of radiation therapy and reduces metastasis of human cancer xenografts in nude rats. Cancer Res. 2010 Oct 1;70(19):7591-9. | ||||
Ref 532993 | Abituzumab combined with cetuximab plus irinotecan versus cetuximab plus irinotecan alone for patients with KRAS wild-type metastatic colorectal cancer: the randomised phase I/II POSEIDON trial. Ann Oncol. 2015 Jan;26(1):132-40. |
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