Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T80782
|
||||
Former ID |
TTDC00334
|
||||
Target Name |
mRNA of VEGFR1
|
||||
Gene Name |
FLT1
|
||||
Synonyms |
mRNA 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; FLT1
|
||||
Target Type |
Clinical Trial
|
||||
Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
Exudative age-related macular degeneration [ICD9: 362.5; ICD10: H35.3] | |||||
Neovascular age-related macular degeneration [ICD9: 362.5; ICD10: H35.3] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Receptorfor 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.
|
||||
BioChemical Class |
Kinase
|
||||
Target Validation |
T80782
|
||||
UniProt ID | |||||
EC Number |
EC 2.7.10.1
|
||||
Sequence |
MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK
WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC CSPPPDYNSVVLYSTPPI |
||||
Drugs and Mode of Action | |||||
Inhibitor | (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [527458] | ||
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine | Drug Info | [527458] | |||
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole | Drug Info | [528122] | |||
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile | Drug Info | [527458] | |||
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine | Drug Info | [526421] | |||
3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile | Drug Info | [527458] | |||
4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide | Drug Info | [527458] | |||
4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine | Drug Info | [527948] | |||
4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine | Drug Info | [527948] | |||
4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
AAL-993 | Drug Info | [528016] | |||
CB-676475 | Drug Info | [530858] | |||
Cdk1/2 inhibitor III | Drug Info | [527600] | |||
compound 25 | Drug Info | [529100] | |||
compound 8h | Drug Info | [531959] | |||
C[homoPhe-Hca-Glu-Gly-Leu-Glu-Glu]-NH2 | Drug Info | [529068] | |||
C[YYAEGLEE]-NH2 | Drug Info | [530908] | |||
C[YYDEGLEE]-NH2 | Drug Info | [530908] | |||
C[YYDEKLEE]-NH2 | Drug Info | [530908] | |||
IM-094261 | Drug Info | [527725] | |||
IM-094882 | Drug Info | [527948] | |||
LYCOGARUBIN B | Drug Info | [527562] | |||
MK-2461 | Drug Info | [530708] | |||
N-(2,4-Dichloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide | Drug Info | [527245] | |||
N3-GHQMFYYPra-NH2 | Drug Info | [529026] | |||
Phenyl-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [527458] | |||
SEMAXINIB | Drug Info | [525812] | |||
VATALANIB | Drug Info | [528016] | |||
[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol | Drug Info | [527458] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Ras signaling pathway | ||||
Rap1 signaling pathway | |||||
Cytokine-cytokine receptor interaction | |||||
HIF-1 signaling pathway | |||||
Endocytosis | |||||
PI3K-Akt signaling pathway | |||||
Focal adhesion | |||||
Transcriptional misregulation in cancer | |||||
Rheumatoid arthritis | |||||
Pathway Interaction Database | Glypican 1 network | ||||
HIF-2-alpha transcription factor network | |||||
S1P3 pathway | |||||
VEGF and VEGFR signaling network | |||||
VEGFR1 specific signals | |||||
Signaling events mediated by VEGFR1 and VEGFR2 | |||||
Reactome | Neurophilin interactions with VEGF and VEGFR | ||||
VEGF binds to VEGFR leading to receptor dimerization | |||||
WikiPathways | Focal Adhesion | ||||
Signaling by VEGF | |||||
Angiogenesis | |||||
References | |||||
Ref 521851 | ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 525812 | J 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. | ||||
Ref 526421 | Bioorg 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. | ||||
Ref 527245 | J 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. | ||||
Ref 527458 | J 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. | ||||
Ref 527562 | Bioorg 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. | ||||
Ref 527600 | 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11. | ||||
Ref 527725 | Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8.Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase. | ||||
Ref 527948 | Bioorg 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. | ||||
Ref 528016 | Bioorg 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. | ||||
Ref 528122 | Bioorg 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. | ||||
Ref 529026 | Bioorg 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. | ||||
Ref 529068 | J 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. | ||||
Ref 529100 | Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6593-601. Epub 2007 Sep 22. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 530858 | Bioorg 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. | ||||
Ref 530908 | J 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. | ||||
Ref 531959 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.