Target Information

Target General Infomation
Target ID
T23355
Former ID
TTDR01362
Target Name
mRNA of integrin beta 3
Gene Name
ITGB3
Synonyms
CD61 (mRNA); GPIIIa (mRNA); ITGB3 (mRNA); Integrin beta3 (mRNA); Platelet membrane glycoprotein IIIa (mRNA); ITGB3
Target Type
Discontinued
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.
BioChemical Class
Integrin
Target Validation
T23355
UniProt ID
P05106
Sequence
MRARPRPRPLWATVLALGALAGVGVGGPNICTTRGVSSCQQCLAVSPMCAWCSDEALPLG
SPRCDLKENLLKDNCAPESIEFPVSEARVLEDRPLSDKGSGDSSQVTQVSPQRIALRLRP
DDSKNFSIQVRQVEDYPVDIYYLMDLSYSMKDDLWSIQNLGTKLATQMRKLTSNLRIGFG
AFVDKPVSPYMYISPPEALENPCYDMKTTCLPMFGYKHVLTLTDQVTRFNEEVKKQSVSR
NRDAPEGGFDAIMQATVCDEKIGWRNDASHLLVFTTDAKTHIALDGRLAGIVQPNDGQCH
VGSDNHYSASTTMDYPSLGLMTEKLSQKNINLIFAVTENVVNLYQNYSELIPGTTVGVLS
MDSSNVLQLIVDAYGKIRSKVELEVRDLPEELSLSFNATCLNNEVIPGLKSCMGLKIGDT
VSFSIEAKVRGCPQEKEKSFTIKPVGFKDSLIVQVTFDCDCACQAQAEPNSHRCNNGNGT
FECGVCRCGPGWLGSQCECSEEDYRPSQQDECSPREGQPVCSQRGECLCGQCVCHSSDFG
KITGKYCECDDFSCVRYKGEMCSGHGQCSCGDCLCDSDWTGYYCNCTTRTDTCMSSNGLL
CSGRGKCECGSCVCIQPGSYGDTCEKCPTCPDACTFKKECVECKKFDRGALHDENTCNRY
CRDEIESVKELKDTGKDAVNCTYKNEDDCVVRFQYYEDSSGKSILYVVEEPECPKGPDIL
VVLLSVMGAILLIGLAALLIWKLLITIHDRKEFAKFEEERARAKWDTANNPLYKEATSTF
TNITYRGT
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 545001Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001842)
Ref 545332Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002874)
Ref 545463Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003353)
Ref 545736Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004434)
Ref 545885Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005208)
Ref 546018Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005906)
Ref 546064Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006161)
Ref 546478Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008429)
Ref 546484Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008466)
Ref 546520Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008713)
Ref 525558J 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 525656J 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 525874J 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 526139Bioorg 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 526893J Med Chem. 2003 Dec 4;46(25):5316-25.Molecular model of the alpha(IIb)beta(3) integrin.
Ref 527223Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Ref 527268Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.
Ref 527440J 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 527884J 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 528059J 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 528111J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Ref 528215J Med Chem. 2006 Jun 1;49(11):3416-20.Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior.
Ref 528383Bioorg 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 528438Bioorg 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 528659Bioorg 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 529045Bioorg 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 529125J Med Chem. 2007 Nov 29;50(24):5878-81. Epub 2007 Nov 1.Multiple N-methylation by a designed approach enhances receptor selectivity.
Ref 529343J 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 530479J Med Chem. 2009 Nov 26;52(22):7029-43.alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers.
Ref 530622J 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 530779J Med Chem. 2010 Jun 10;53(11):4332-53.Emerging targets in osteoporosis disease modification.
Ref 533764J Med Chem. 1995 Jan 6;38(1):34-41.Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation.
Ref 534458J 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 534805Bioorg 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 549674US patent application no. 7,425,545, Modulation of C-reactive protein expression.
Ref 551258Preparation 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).
Ref 551268Non-peptide fibrinogen receptor antagonists. 3. design and discovery of a centrally constrained inhibitorc, Bioorg. Med. Chem. Lett. 4(15):1835-1840 (1994).
Ref 551284Synthesis and antiplatelet activity of DMP 757 analogs, Bioorg. Med. Chem. Lett. 5(18):2097-2100 (1995).

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