Therapeutic Targets Database
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TTD Target ID: TTDR01362

Target Information
NamemRNA of integrin beta 3    
Type of targetResearch target    
DiseaseNot Available
UniProt IDP05106
PDB Structure1JV2; 1KUP; 1KUZ; 1L5G; 1M1X; 1M8O; 1MK7; 1MK9; 1RN0; 1S4X; 1TYE; 1U8C; 2INI; 2K9J; 2KNC; 2KV9; 2L1C; 2L91; 2LJD; 2LJE; 2LJF; 2Q6W; 2RMZ; 2RN0; 2VC2; 2VDK; 2VDL; 2VDM; 2VDN; 2VDO; 2VDP; 2VDQ; 2VDR; 3FCS; 3FCU; 3IJE; 3NID; 3NIF; 3NIG; 3T3M; 3T3P; 3ZDX; 3ZDY; 3ZDZ; 3ZE0; 3ZE1; 3ZE2; 4G1E; 4G1M.    
Target ValidationClick to Find Target Validation Information.    
Inhibitor3- (3-[1]
3- (3-[1]
3- (3-[1]
Ac-Asp-Arg-Leu-Asp-Ser-OH[2]
AcDRGDS[3]
CYCLORGDFV[4]
DMP-728[5]
DMP-757[6]
DMP-802[5]
ELAROFIBAN[7]
E[c (RGDyK)]2[8]
E[c (RGDyK)]2-PTX conjugate[8]
FK-633[5]
GR-144053,   GR-144053F[5]
Gantofiban[5]
Gly-Arg-Gly-Asp-Ser[9]
Gly-Arg-Gly-Asp-Ser-Pro-Lys[10]
ISONIPECOTAMIDE[7]
L-703014[5]
L-709780[11]
L-734115[5]
L-734217[12]
L-738167[5]
L-739758[5]
L-746233[5]
L-750034[13]
L-756568[5]
L-767679[5]
LAMIFIBAN[5]
LOTRAFIBAN[5]
MK-852[5]
N- (3,5-dichlorophenyl)imidodicarbonimidic diamide[14]
ORBOFIBAN[5]
RGDechi[15]
RO-44-3888[5]
ROXIFIBAN[5]
RWJ-53419[16]
Ro-43-5054[5]
Ro-43-8857[5]
SB-207043[17]
SB-208651[18]
SB-223245[19]
SB-265123[20]
SC-47643[21]
SC-54701A[22]
SIBRAFIBAN[5]
SKF-106760[23]
SKF-107260[17]
ST-1646[24]
XEMILOFIBAN[25]
ZD-2486[5]
c (-GRGDfL-)[26]
c (Arg-Gly-Asp-D-Phe-Val)[15]
c (RGDfF)[27]
c (RGDfMeF)[27]
c (RGDfV)[28]
c-[-Arg-Gly-Asp-Acpca30-][29]
c-[-Arg-Gly-Asp-Acpca31-][29]
c-[-Arg-Gly-Asp-Acpca32-][29]
c-[-Arg-Gly-Asp-Acpca33-][29]
c[-Arg-Gly-Asp-Acpca19-][29]
c[-Arg-Gly-Asp-Acpca20-][29]
c[-Arg-Gly-Asp-Acpca21-][29]
c[-Arg-Gly-Asp-Acpca22-][29]
c[-Arg-Gly-Asp-Acpca34-][29]
c[-Arg-Gly-Asp-Acpca35-][29]
c[-Arg-Gly-Asp-Acpca36-][29]
c[RGD- (R)-alpha-TfmfV][27]
c[RGD- (S)-alpha-TfmfV][27]
c[RGDf- (R)-N-Me-alpha-TfmF][27]
c[RGDf- (R)-alpha-TfmF][27]
c[RGDf- (R)-alpha-TfmV][27]
c[RGDf- (S)-N-Me-alpha-TfmF][27]
c[RGDf- (S)-alpha-TfmF][27]
c[RGDf- (S)-alpha-TfmV][27]
c[RGDf- (S,R)-alpha-Dfm-F][27]
cyclo (RGDfV) [30]
cyclo-[-Arg-Gly-Asp-Amp21-][24]
cyclo-[-Arg-Gly-Asp-Amp22-][24]
cyclo-[-Arg-Gly-Asp-Amp23-][24]
cyclo-[-Arg-Gly-Asp-Amp24-][24]
cyclo-[-Arg-Gly-Asp-Amp25-][24]
cyclo-[-Arg-Gly-Asp-Amp26-][24]
cyclo-[-Arg-Gly-Asp-Amp27-][24]
cyclo-[-Arg-Gly-Asp-Amp28-][24]
cyclo[RGDfK (cypate)][30]
cypate-[ (RGD)2-NH2]1[30]
cypate-[ (RGD)2-NH2]2[30]
cypate-[ (RGD)3-NH2]1[30]
cypate-[ (RGD)3-NH2]2[30]
cypate-[ (RGD)4-NH2]1[30]
cypate-[ (RGD)4-NH2]2[30]
AntisenseISIS 196103[31]
ISIS 25237[31]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Bioorg 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. To Reference
Ref 2Bioorg 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. To Reference
Ref 3Bioorg 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. To Reference
Ref 4J 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. To Reference
Ref 5J 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. To Reference
Ref 6Bioorg. Med. Chem. Lett. 5(18):2097-2100 (1995) To Reference
Ref 7Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins. To Reference
Ref 8J 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. To Reference
Ref 9J Med Chem. 2009 Nov 26;52(22):7029-43.alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers. To Reference
Ref 10J 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. To Reference
Ref 11Bioorg. Med. Chem. Lett. 4(15):1835-1840 (1994) To Reference
Ref 12Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8.Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors. To Reference
Ref 13J Med Chem. 2003 Dec 4;46(25):5316-25.Molecular model of the alpha(IIb)beta(3) integrin. To Reference
Ref 14J Med Chem. 2010 Jun 10;53(11):4332-53.Emerging targets in osteoporosis disease modification. To Reference
Ref 15J Med Chem. 2006 Jun 1;49(11):3416-20.Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior. To Reference
Ref 16Bioorg 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. To Reference
Ref 17Bioorg. Med. Chem. Lett. 3(6):1179-1184 (1993) To Reference
Ref 18J Med Chem. 1999 Feb 25;42(4):545-59.Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists. To Reference
Ref 19Bioorg 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. To Reference
Ref 20Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability. To Reference
Ref 21J Med Chem. 1995 Jan 6;38(1):34-41.Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation. To Reference
Ref 22J 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. To Reference
Ref 23J Med Chem. 1992 Oct 16;35(21):3970-2.Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists. To Reference
Ref 24J 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. To Reference
Ref 25J 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. To Reference
Ref 26J Med Chem. 2007 Nov 29;50(24):5878-81. Epub 2007 Nov 1.Multiple N-methylation by a designed approach enhances receptor selectivity. To Reference
Ref 27J 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. To Reference
Ref 28Bioorg 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. To Reference
Ref 29J 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. To Reference
Ref 30J Med Chem. 2006 Apr 6;49(7):2268-75.Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors. To Reference
Ref 31US Patent 7425545 To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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