Therapeutic Targets Database
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TTD Target ID: TTDS00007

Target Information
NameVascular endothelial growth factor receptor 1    
Type of targetSuccessful target    
SynonymsFlt-1    
Fms-like tyrosine kinase 1    
Tyrosine-protein kinase FRT    
Tyrosine-protein kinase receptor FLT    
VEGFR-1    
Vascular permeability factor receptor    
DiseaseAngiogenesis[1]
Angiogenesis in metastatic and atherosclerotic processes[2]
Inflammatory diseases[1]
Drug(s)RanibizumabApprovedAge-related macular degeneration[3]
SorafenibLaunchedAdvanced renal cell carcinoma[4][5][6]
ASP4130US Filed; Europe Phase-IIIAdvanced renal cell carcinoma
BrivanibPhase IIIFirst-line liver cancer, liver cancer (TACE) (see also colorectal, sarcoma)
NintedanibPhase IIINon-small cell lung cancer (NSCLC)
NintedanibPhase IIIOvarian cancer
RanibizumabPhase IIIDiabetic macular edema and retinal vein occlusion[3][7]
SorafenibPhase IIIHepatocellular carcinoma, NSCLC, melanoma[4][5][6]
BrivanibPhase IIMetastatic colorectal cancer
BrivanibPhase IISarcoma
LY3012212Phase IIBladder cancer
SorafenibPhase IIMyelodyspalstic syndrome, AML, head & neck cancer, breast, colon, ovarian, pancreatic cancer[4][5][6]
CEP-11981Phase I completedSolid Tumors
X-82Phase IAdvanced solid tumors
TelberminDiscontinued in Phase IIDiabetic foot ulcers[8]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayCytokine-cytokine receptor interaction
Focal adhesion
UniProt IDP17948
PDB Structure1FLT; 1QSV; 1QSZ; 1QTY; 1RV6; 2XAC; 3HNG.    
FunctionReceptor for VEGF, VEGFB and PGF, and has a tyrosine-protein kinase activity. The VEGF-kinase ligand/receptor signaling system plays a key role in vascular development and regulation of vascular permeability.    
SequenceMVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC CSPPPDYNSVVLYSTPPI
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorAAL-993[9]
Ranibizumab[3][7]
Ranibizumab[3]
SEMAXINIB[9]
SU-11652[10]
SU-5416[11]
Sorafenib[4][5][6]
ActivatorTelbermin[8]
MultitargetSorafenib[4][5][6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Placental growth factor and its receptor, vascular endothelial growth factor receptor-1: novel targets for stimulation of ischemic tissue revascularization and inhibition of angiogenic and inflammatory disorders. J Thromb Haemost. 2003 Jul;1(7):1356-70. To Reference
Ref 2Inhibition of vascular endothelial growth factor (VEGF) as a novel approach for cancer therapy. Medicina (B Aires). 2000;60 Suppl 2:41-7. To Reference
Ref 3The Effect of Intravitreal Ranibizumab on the Fellow Untreated Eye with Subfoveal Scarring due to Exudative Age-Related Macular Degeneration. Ophthalmologica. 2009 Jul 15;223(6):383-389. [Epub ahead of print] To Reference
Ref 4A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 5Pituitary tumors. Curr Treat Options Neurol. 2009 Jul;11(4):287-96. To Reference
Ref 6Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 7Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 8Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. To Reference
Ref 9J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. To Reference
Ref 10J 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
Ref 11Antiangiogenic effect by SU5416 is partly attributable to inhibition of Flt-1 receptor signaling. Mol Cancer Ther. 2002 Mar;1(5):295-302. To Reference



 

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