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
P17948
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
Drug(s) VATALANIB Drug Info Phase 2 Solid tumours [521851], [541046]
MK-2461 Drug Info Phase 1/2 Alzheimer disease [530708]
Sirna-027 Drug Info Phase 1/2 Exudative age-related macular degeneration [551694]
Sirna-027 Drug Info Phase 1 Neovascular age-related macular degeneration [551694]
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 521851ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health.
Ref 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 541046(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5705).
Ref 5516942011 Pipeline of Sirna Therapeutics.
Ref 525812J 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 526421Bioorg 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 527245J 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 527458J 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 527562Bioorg 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 5276001-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 527725Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8.Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.
Ref 527948Bioorg 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 528016Bioorg 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 528122Bioorg 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 529026Bioorg 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 529068J 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 529100Macrocyclic 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 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 530858Bioorg 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 530908J 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 531959The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
Ref 536057Future pharmacological treatment options for nonexudative and exudative age-related macular degeneration. Expert Opin Emerg Drugs. 2005 Feb;10(1):119-35.
Ref 5516942011 Pipeline of Sirna Therapeutics.

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