Therapeutic Targets Database
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TTD Target ID: TTDC00311

Target Information
NameAlpha platelet-derived growth factor receptor    
Type of targetDiscontinued target    
SynonymsCD140a antigen    
PDGF-R-alpha    
Platelet-derived growth factor receptor alpha    
DiseaseHypereosinophilic syndrome
[ICD9: 288.3   ICD10: D72.1]
[1]
Lung cancer
[ICD9: 162   ICD10: C33-C34]
[2]
Drug(s)MEDI-575Phase IIGlioblastoma[3]
OlaratumabPhase IINon-small cell lung cancer
TAK-593Discontined in Phase ISolid tumors[4]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayCalcium signaling pathway
Colorectal cancer
Cytokine-cytokine receptor interaction
Focal adhesion
Gap junction
Glioma
MAPK signaling pathway
Melanoma
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
UniProt IDP16234
PDB Structure1GQ5.    
FunctionReceptor that binds both pdgfa and pdgfb and has a tyrosine-protein kinase activity.    
SequenceMGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYP MSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIY VPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNG TFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNN EVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVK EMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENL TEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDL VDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRD RSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVII SLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLG SGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNL LGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSY VILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKN LLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLA RDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMM VDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKK SYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYII PLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDS SDLVEDSFL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1H-indol-2-yl)[5]
(1H-indol-2-yl)[5]
(1H-indol-2-yl)[5]
(5-fluoro-1H-indol-2-yl)-[5]
(5-hydroxy-1H-indol-2-yl)[5]
1-Phenyl-1H-benzoimidazol-5-ol[6]
1-Phenyl-1H-benzoimidazole[6]
3- ([7]
3- (1H-Indol-3-yl)-6,7-dimethoxy-quinoline[7]
3- (1H-Indol-3-yl)-quinoline[7]
3- (2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline[7]
3- (3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline[7]
3- (3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline[7]
3- (3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline[7]
3- (3-Fluoro-phenyl)-6,7-dimethoxy-quinoline[7]
3- (4-Fluoro-phenyl)-6,7-dimethoxy-quinoline[7]
3-Benzyloxy-6,7-dimethoxy-quinoline[7]
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline[7]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline[7]
3-Cyclopentyl-6,7-dimethoxy-quinoline[7]
3-Pyridin-3-yl-quinoline-6,7-diol[7]
3-Pyridin-4-yl-quinolin-7-ol[8]
3-Pyridin-4-yl-quinoline[8]
3-Pyridin-4-yl-quinoline-5,7-diol[8]
3-Thiophen-3-yl-quinoline[7]
4- (3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline[9]
4- (5-Methoxy-benzoimidazol-1-yl)-phenylamine[10]
4- (6,7-Dimethoxy-quinolin-3-yl)-benzoic acid[7]
4- (6,7-Dimethoxy-quinolin-3-yl)-phenol[7]
4-Benzoimidazol-1-yl-phenylamine[6]
5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol[11]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline[8]
5,7-Dimethoxy-3-pyridin-4-yl-quinoline[8]
5,7-Dimethoxy-3-thiophen-3-yl-quinoline[7]
5,7-Dimethyl-3-thiophen-3-yl-quinoline[7]
5- (6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one[7]
5-Fluoro-3-thiophen-3-yl-quinoline[7]
5-Methoxy-1-phenyl-1H-benzoimidazole[6]
6,7-Dichloro-3-thiophen-3-yl-quinoline[7]
6,7-Difluoro-3-thiophen-3-yl-quinoline[7]
6,7-Dimethoxy-3- ([7]
6,7-Dimethoxy-3- (2-methoxy-phenyl)-quinoline[7]
6,7-Dimethoxy-3- (3-methoxy-phenyl)-quinoline[7]
6,7-Dimethoxy-3- (4-methoxy-phenyl)-quinoline[7]
6,7-Dimethoxy-3- (4-nitro-phenyl)-quinoline[7]
6,7-Dimethoxy-3-p-tolyl-quinoline[7]
6,7-Dimethoxy-3-phenyl-quinoline[7]
6,7-Dimethoxy-3-phenylethynyl-quinoline[7]
6,7-Dimethoxy-3-pyridin-3-yl-quinoline[7]
6,7-Dimethoxy-3-pyridin-4-yl-quinoline[8]
6,7-Dimethoxy-3-thiophen-2-yl-quinoline[7]
6-Methoxy-3-pyridin-4-yl-quinoline[8]
6-Methoxy-3-thiophen-3-yl-quinoline[7]
7-Chloro-3-pyridin-4-yl-quinoline[8]
7-Fluoro-3-thiophen-3-yl-quinoline[7]
7-Methoxy-3-pyridin-4-yl-quinoline[8]
7-Methoxy-3-thiophen-3-yl-quinoline[7]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline[7]
AG1295[5]
AZD-0530[12]
BMS-536924[13]
Benzyl- (6,7-dimethoxy-quinolin-3-yl)-amine[7]
Bis- (5-hydroxy-1H-indol-2-yl)-methanone[5]
ELLIPTINIUM[11]
JNJ-10198409[14]
PD-0166326,   PD-166326[15]
PD-0173952[15]
PD-0173955,   PD-17395[15]
PD-0173956[15]
PD-0173958[15]
PD-0179483[15]
PD-0180970[15]
PD-173074[16]
RG-13022[7]
RPR-101511[7]
RPR-108514A[17]
Ro-4396686[18]
SEMAXINIB[19]
SU-11652[19]
TAK-593[4]
di (1H-indol-2-yl)methanone[5]
AntibodyMEDI-575[3]
MultitargetTAK-593[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Molecular remission and reversal of myelofibrosis in response to imatinib mesylate treatment in patients with the myeloproliferative variant of hypereosinophilic syndrome. Blood. 2004 Jan 15;103(2):473-8. Epub 2003 Sep 22. To Reference
Ref 2Gleevec (STI-571) inhibits lung cancer cell growth (A549) and potentiates the cisplatin effect in vitro. Mol Cancer. 2003 Jan 3;2:1. To Reference
Ref 32011 Pipeline of MedImmune. To Reference
Ref 4Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 5J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 6J Med Chem. 1998 Dec 31;41(27):5457-65.Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor. To Reference
Ref 7J Med Chem. 1994 Jul 8;37(14):2129-37.A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives. To Reference
Ref 8J Med Chem. 1994 Aug 19;37(17):2627-9.5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 9Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997) To Reference
Ref 10J Med Chem. 1999 Jul 1;42(13):2373-82.Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor. To Reference
Ref 11J Med Chem. 2005 Oct 6;48(20):6194-201.Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. To Reference
Ref 12J Med Chem. 2006 Nov 2;49(22):6465-88.N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. To Reference
Ref 13J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. To Reference
Ref 14J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. To Reference
Ref 15Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. To Reference
Ref 16J Med Chem. 2005 Jul 14;48(14):4628-53.Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. To Reference
Ref 17Bioorg. Med. Chem. Lett. 7(4):421-424 (1997) To Reference
Ref 18Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. To Reference
Ref 19J Med Chem. 2003 Mar 27;46(7):1116-9.Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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