Target Information
Target General Infomation | |||||
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Target ID |
T23355
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Former ID |
TTDR01362
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Target Name |
mRNA of integrin beta 3
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Gene Name |
ITGB3
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Synonyms |
CD61 (mRNA); GPIIIa (mRNA); ITGB3 (mRNA); Integrin beta3 (mRNA); Platelet membrane glycoprotein IIIa (mRNA); ITGB3
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Target Type |
Discontinued
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Disease | Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9] | ||||
Function |
Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha-V/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha- IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha- IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets (By similarity). In case of HIV-1 infection, the interaction with extracellular viral Tat protein seems to enhance angiogenesis in Kaposi's sarcoma lesions.
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BioChemical Class |
Integrin
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Target Validation |
T23355
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UniProt ID | |||||
Sequence |
MRARPRPRPLWATVLALGALAGVGVGGPNICTTRGVSSCQQCLAVSPMCAWCSDEALPLG
SPRCDLKENLLKDNCAPESIEFPVSEARVLEDRPLSDKGSGDSSQVTQVSPQRIALRLRP DDSKNFSIQVRQVEDYPVDIYYLMDLSYSMKDDLWSIQNLGTKLATQMRKLTSNLRIGFG AFVDKPVSPYMYISPPEALENPCYDMKTTCLPMFGYKHVLTLTDQVTRFNEEVKKQSVSR NRDAPEGGFDAIMQATVCDEKIGWRNDASHLLVFTTDAKTHIALDGRLAGIVQPNDGQCH VGSDNHYSASTTMDYPSLGLMTEKLSQKNINLIFAVTENVVNLYQNYSELIPGTTVGVLS MDSSNVLQLIVDAYGKIRSKVELEVRDLPEELSLSFNATCLNNEVIPGLKSCMGLKIGDT VSFSIEAKVRGCPQEKEKSFTIKPVGFKDSLIVQVTFDCDCACQAQAEPNSHRCNNGNGT FECGVCRCGPGWLGSQCECSEEDYRPSQQDECSPREGQPVCSQRGECLCGQCVCHSSDFG KITGKYCECDDFSCVRYKGEMCSGHGQCSCGDCLCDSDWTGYYCNCTTRTDTCMSSNGLL CSGRGKCECGSCVCIQPGSYGDTCEKCPTCPDACTFKKECVECKKFDRGALHDENTCNRY CRDEIESVKELKDTGKDAVNCTYKNEDDCVVRFQYYEDSSGKSILYVVEEPECPKGPDIL VVLLSVMGAILLIGLAALLIWKLLITIHDRKEFAKFEEERARAKWDTANNPLYKEATSTF TNITYRGT |
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Drugs and Mode of Action | |||||
Drug(s) | XEMILOFIBAN | Drug Info | Discontinued in Phase 3 | Peripheral vascular disease | [545736] |
DMP-802 | Drug Info | Discontinued in Phase 1 | Discovery agent | [546484] | |
DMP-757 | Drug Info | Terminated | Discovery agent | [546018] | |
L-709780 | Drug Info | Terminated | Discovery agent | [545885] | |
L-738167 | Drug Info | Terminated | Discovery agent | [546520] | |
Ro-43-5054 | Drug Info | Terminated | Discovery agent | [545001] | |
Ro-43-8857 | Drug Info | Terminated | Discovery agent | [546064] | |
SB-223245 | Drug Info | Terminated | Discovery agent | [546478] | |
SC-47643 | Drug Info | Terminated | Discovery agent | [545332] | |
SKF-107260 | Drug Info | Terminated | Discovery agent | [545463] | |
Inhibitor | 3-(3-(benzamido)-5-nitrobenzamido)propanoic acid | Drug Info | [528383] | ||
3-(3-(carbamoyl)benzamido)-3-phenylpropanoic acid | Drug Info | [528383] | |||
3-(3-(carbamoyl)benzamido)propanoic acid | Drug Info | [528383] | |||
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-(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] | |||
DMP-757 | Drug Info | [551284] | |||
DMP-802 | Drug Info | [525874] | |||
E[c(RGDyK)]2 | Drug Info | [527440] | |||
E[c(RGDyK)]2-PTX conjugate | Drug Info | [527440] | |||
Gly-Arg-Gly-Asp-Ser | Drug Info | [530479] | |||
Gly-Arg-Gly-Asp-Ser-Pro-Lys | Drug Info | [525558] | |||
ISONIPECOTAMIDE | Drug Info | [527223] | |||
L-709780 | Drug Info | [551268] | |||
L-734115 | Drug Info | [525874] | |||
L-738167 | Drug Info | [525874] | |||
L-739758 | Drug Info | [525874] | |||
L-746233 | Drug Info | [525874] | |||
L-750034 | Drug Info | [526893] | |||
L-756568 | Drug Info | [525874] | |||
L-767679 | Drug Info | [525874] | |||
N-(3,5-dichlorophenyl)imidodicarbonimidic diamide | Drug Info | [530779] | |||
RGDechi | Drug Info | [528215] | |||
Ro-43-5054 | Drug Info | [525874] | |||
Ro-43-8857 | Drug Info | [525874] | |||
ROXIFIBAN | Drug Info | [525874] | |||
RWJ-53419 | Drug Info | [526139] | |||
SB-207043 | Drug Info | [551258] | |||
SB-223245 | Drug Info | [534805] | |||
SB-265123 | Drug Info | [527268] | |||
SC-47643 | Drug Info | [533764] | |||
SC-54701A | Drug Info | [534458] | |||
SKF-107260 | Drug Info | [551258] | |||
ST-1646 | Drug Info | [529343] | |||
XEMILOFIBAN | Drug Info | [525656] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Rap1 signaling pathway | ||||
Phagosome | |||||
PI3K-Akt signaling pathway | |||||
Osteoclast differentiation | |||||
Focal adhesion | |||||
ECM-receptor interaction | |||||
Platelet activation | |||||
Hematopoietic cell lineage | |||||
Regulation of actin cytoskeleton | |||||
Thyroid hormone signaling pathway | |||||
Proteoglycans in cancer | |||||
MicroRNAs in cancer | |||||
Hypertrophic cardiomyopathy (HCM) | |||||
Arrhythmogenic right ventricular cardiomyopathy (ARVC) | |||||
Dilated cardiomyopathy | |||||
NetPath Pathway | Leptin Signaling Pathway | ||||
Pathway Interaction Database | IL4-mediated signaling events | ||||
Integrin family cell surface interactions | |||||
Signaling events mediated by PTP1B | |||||
Beta3 integrin cell surface interactions | |||||
S1P3 pathway | |||||
Osteopontin-mediated events | |||||
Nectin adhesion pathway | |||||
Arf6 signaling events | |||||
S1P1 pathway | |||||
Integrins in angiogenesis | |||||
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
PDGFR-beta signaling pathway | |||||
Signaling events mediated by VEGFR1 and VEGFR2 | |||||
Ephrin B reverse signaling | |||||
Reactome | Platelet degranulation | ||||
Elastic fibre formation | |||||
PECAM1 interactions | |||||
Molecules associated with elastic fibres | |||||
Integrin cell surface interactions | |||||
Syndecan interactions | |||||
ECM proteoglycans | |||||
Integrin alphaIIb beta3 signaling | |||||
SOS provides linkage to MAPK signaling for Integrins | |||||
p130Cas linkage to MAPK signaling for integrins | |||||
VEGFA-VEGFR2 Pathway | |||||
MAP2K and MAPK activation | |||||
WikiPathways | Monoamine Transport | ||||
TGF beta Signaling Pathway | |||||
Osteoblast Signaling | |||||
Focal Adhesion | |||||
Hematopoietic Stem Cell Differentiation | |||||
Human Complement System | |||||
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 | |||||
Integrin alphaIIb beta3 signaling | |||||
Cell surface interactions at the vascular wall | |||||
Serotonin Transporter Activity | |||||
Osteopontin Signaling | |||||
Osteoclast Signaling | |||||
References | |||||
Ref 545001 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001842) | ||||
Ref 545332 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002874) | ||||
Ref 545463 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003353) | ||||
Ref 545736 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004434) | ||||
Ref 545885 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005208) | ||||
Ref 546018 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005906) | ||||
Ref 546064 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006161) | ||||
Ref 546478 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008429) | ||||
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 525656 | J Med Chem. 1999 Dec 16;42(25):5254-65.Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308. | ||||
Ref 525874 | J Med Chem. 2000 Sep 21;43(19):3453-73.Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. | ||||
Ref 526139 | Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22.1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) 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 528383 | Bioorg Med Chem Lett. 2006 Oct 15;16(20):5294-7. Epub 2006 Aug 21.Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists. | ||||
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 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 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 533764 | J Med Chem. 1995 Jan 6;38(1):34-41.Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation. | ||||
Ref 534458 | J Med Chem. 1997 Aug 29;40(18):2843-57.Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists. | ||||
Ref 534805 | Bioorg Med Chem Lett. 1998 Nov 17;8(22):3171-6.Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model. | ||||
Ref 551258 | Preparation and Properties of a fibrinogen receptor antagonist containing the Arg-Gly-Asp sequence and nitroxide radicals, Bioorg. Med. Chem. Lett. 3(6):1179-1184 (1993). |
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