Therapeutic Targets Database
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TTD Target ID: TTDC00334

Target Information
NamemRNA of VEGFR1    
Type of targetClinical trial target    
SynonymsmRNA of FLT-1    
mRNA of FLT1    
mRNA of Fms-like tyrosine kinase 1    
mRNA of Tyrosine-protein kinase FRT    
mRNA of Tyrosine-protein kinase receptor FLT    
mRNA of VEGFR-1    
mRNA of Vascular endothelial growth factor receptor 1    
mRNA of Vascular permeability factor receptor    
DiseaseExudative age-related macular degeneration
[ICD9: 362.50   ICD10: H35.3]
[1]
Neovascular Age-Related Macular Degeneration
[ICD9: 362.50   ICD10: H35.3]
[1]
Drug(s)Sirna-027Phase I/II completedExudative age-related macular degeneration[1][2]
Sirna-027Phase INeovascular Age-Related Macular Degeneration[1][2]
UniProt IDP17948
PDB Structure1FLT; 1QSV; 1QSZ; 1QTY; 1RV6; 2XAC; 3HNG.    
FunctionReceptor for VEGF, VEGFB and PGF. 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. Isoform SFlt1 may have an inhibitory role in angiogenesis.    
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.    
Inhibitor (2-Methoxy-phenyl)-[3]
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine[3]
2- (1H-indazol-3-yl)-1H-benzo[d]imidazole[4]
2- (5-Phenyl-oxazol-2-ylamino)-benzonitrile[3]
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine[5]
3- (5-Phenyl-oxazol-2-ylamino)-benzonitrile[3]
4- (5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide[3]
4- (isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine[6]
4- (isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine[6]
4-Chloro-N- (2-chloro-benzoyl)-benzenesulfonamide[7]
4-Chloro-N- (2-methyl-benzoyl)-benzenesulfonamide[7]
4-Chloro-N- (3-chloro-benzoyl)-benzenesulfonamide[7]
4-Chloro-N- (4-chloro-benzoyl)-benzenesulfonamide[7]
4-Chloro-N- (4-nitro-benzoyl)-benzenesulfonamide[7]
AAL-993[8]
BMS-540215[9]
CB-676475[10]
IM-094261[11]
IM-094882[6]
LYCOGARUBIN B[12]
N- (2,4-Dichloro-benzoyl)-benzenesulfonamide[7]
N- (3-Bromo-benzoyl)-4-chloro-benzenesulfonamide[7]
N3-GHQMFYYPra-NH2[13]
PD-173074[14]
Phenyl- (5-phenyl-oxazol-2-yl)-amine[3]
SEMAXINIB[15]
VATALANIB[8]
[3- (5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol[3]
c[YYAEGLEE]-NH2[16]
c[YYDEGLEE]-NH2[16]
c[YYDEKLEE]-NH2[16]
c[homoPhe-Hca-Glu-Gly-Leu-Glu-Glu]-NH2[17]
siRNASirna-027[1][2]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 12011 Pipeline of Sirna Therapeutics. To Reference
Ref 2Future pharmacological treatment options for nonexudative and exudative age-related macular degeneration. Expert Opin Emerg Drugs. 2005 Feb;10(1):119-35. To Reference
Ref 3J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. To Reference
Ref 4Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. To Reference
Ref 5Bioorg Med Chem Lett. 2002 Oct 7;12(19):2767-70.Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors. To Reference
Ref 6Bioorg Med Chem Lett. 2006 Mar 15;16(6):1579-81. Epub 2005 Dec 28.Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II. To Reference
Ref 7J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. To Reference
Ref 8Bioorg Med Chem Lett. 2006 Apr 1;16(7):1913-9. Epub 2006 Feb 3.Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template. To Reference
Ref 9J Med Chem. 2006 Apr 6;49(7):2143-6.Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. To Reference
Ref 10Bioorg Med Chem. 2010 May 15;18(10):3575-87. Epub 2010 Mar 27.Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. To Reference
Ref 11Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8.Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase. To Reference
Ref 12Bioorg Med Chem Lett. 2005 Jun 2;15(11):2776-80.New cytotoxic bisindole alkaloids with protein tyrosine kinase inhibitory activity from a myxomycete Lycogala epidendrum. To Reference
Ref 13Bioorg Med Chem Lett. 2007 Oct 15;17(20):5590-4. Epub 2007 Aug 22.On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition. To Reference
Ref 14J 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 15J Med Chem. 2000 Jun 15;43(12):2310-23.New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. To Reference
Ref 16J Med Chem. 2010 Jun 10;53(11):4428-40.Biochemical and structural analysis of the binding determinants of a vascular endothelial growth factor receptor peptidic antagonist. To Reference
Ref 17J Med Chem. 2007 Oct 18;50(21):5135-46. Epub 2007 Sep 27.Rational design, structure, and biological evaluation of cyclic peptides mimicking the vascular endothelial growth factor. To Reference



 

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