Target Information
Target General Infomation | |||||
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Target ID |
T63966
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Former ID |
TTDS00007
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Target Name |
Vascular endothelial growth factor receptor 1
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Gene Name |
FLT1
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Synonyms |
VEGFR-1; VEGFR1; Fms-like tyrosine kinase 1; FLT-1; Tyrosine-protein kinase FRT; Tyrosine-protein kinase receptor FLT; FLT; Vascular permeability factor receptor; FRT; VEGF-1 receptor; FLT1
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Target Type |
Clinical Trial
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Disease | Arteriosclerosis; Bladder cancer [ICD9:440, 188; ICD10: I70, C67] | ||||
Advanced solid tumor; Macular degeneration [ICD9:140-199, 362.5; ICD10: C00-C75, C7A, C7B, H35.3] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89] | |||||
Hereditary hemorrhagic telangiectasia [ICD10: I78.0] | |||||
Idiopathic pulmonary fibrosis; Non-small cell lung cancer [ICD9:516.3; ICD10: J84.1, C33-C34] | |||||
Ovarian cancer [ICD9: 183; ICD10: C56] | |||||
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9] | |||||
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25] | |||||
Renal cancer [ICD9: 140-229, 189; ICD10: C64] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Receptor 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.
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BioChemical Class |
Kinase
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Target Validation |
T63966
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK
WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC CSPPPDYNSVVLYSTPPI |
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Drugs and Mode of Action | |||||
Drug(s) | Nintedanib | Drug Info | Approved | Idiopathic pulmonary fibrosis | [556264] |
Ranibizumab | Drug Info | Approved | Hereditary hemorrhagic telangiectasia | [528395], [541859] | |
E-3810 | Drug Info | Phase 3 | Solid tumours | [524749], [542632] | |
Fruquintinib | Drug Info | Phase 3 | Cancer | [525024] | |
Nintedanib | Drug Info | Phase 3 | Non-small cell lung cancer | [524516], [524899], [541221] | |
Tivozanib | Drug Info | Phase 3 | Renal cancer | [522960], [541307] | |
Famitinib | Drug Info | Phase 2 | Cancer | [532104], [542811] | |
LY3012212 | Drug Info | Phase 2 | Arteriosclerosis; Bladder cancer | [548347] | |
Nintedanib | Drug Info | Phase 2 | Ovarian cancer | [523930], [541221] | |
OCV-101 | Drug Info | Phase 2 | Pancreatic cancer | [548991] | |
OTSGC-A24 | Drug Info | Phase 1/2 | Colorectal cancer | [523227] | |
CEP-11981 | Drug Info | Phase 1 | Solid tumours | [522626], [542989] | |
EW-A-401 | Drug Info | Phase 1 | Peripheral vascular disease | [521594] | |
Sulfatinib | Drug Info | Phase 1 | Cancer | [524745] | |
X-82 | Drug Info | Phase 1 | Advanced solid tumor; Macular degeneration | [551750] | |
Angiozyme | Drug Info | Discontinued in Phase 2 | Cancer | [546650] | |
Telbermin | Drug Info | Discontinued in Phase 2 | Diabetic foot ulcer | [536297] | |
Inhibitor | AAL-993 | Drug Info | [526484] | ||
E-3810 | Drug Info | [525382] | |||
Famitinib | Drug Info | [532104] | |||
Fruquintinib | Drug Info | [533061] | |||
SEMAXINIB | Drug Info | [526484] | |||
SU-11652 | Drug Info | [526575] | |||
Sulfatinib | Drug Info | [550989] | |||
Tivozanib | Drug Info | [541307] | |||
Modulator | Angiozyme | Drug Info | |||
CEP-11981 | Drug Info | [542989] | |||
EW-A-401 | Drug Info | ||||
LY3012212 | Drug Info | [532445] | |||
Nintedanib | Drug Info | [533123] | |||
OCV-101 | Drug Info | ||||
X-82 | Drug Info | [550468] | |||
Activator | Telbermin | Drug Info | [536297] | ||
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 521594 | ClinicalTrials.gov (NCT00080392) EW-A-401 to Treat Intermittent Claudication. U.S. National Institutes of Health. | ||||
Ref 522626 | ClinicalTrials.gov (NCT00875264) Open-Label Study to Determine the Maximum Tolerated Oral Dose of the Kinase Inhibitor CEP-11981 in Patients With Advanced Cancer. U.S. National Institutes of Health. | ||||
Ref 522960 | ClinicalTrials.gov (NCT01076010) An Extension Treatment Protocol for Subjects Who Have Participated in a Phase 3 Study of Tivozanib Versus Sorafenib in Renal Cell Carcinoma (Protocol AV-951-09-301). U.S. National Institutes of Health. | ||||
Ref 523227 | ClinicalTrials.gov (NCT01227772) Study of OTSGC-A24 Vaccine in Advanced Gastric Cancer. U.S. National Institutes of Health. | ||||
Ref 523930 | ClinicalTrials.gov (NCT01610869) Low Dose Cyclophosphamide +/-- Nintedanib in Advanced Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 524516 | ClinicalTrials.gov (NCT01979952) Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF). U.S. National Institutes of Health. | ||||
Ref 524745 | ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524749 | ClinicalTrials.gov (NCT02135107) A Double-blind Comparative Study of the Efficacy and Safety of E3810 10mg Once and Twice Daily in Maintenance Therapy for PPI Resistant Gastroesophageal Reflux Disease Patients. U.S. National Institutes of Health. | ||||
Ref 524899 | ClinicalTrials.gov (NCT02231164) LUME-Columbus: Nintedanib Plus Docetaxel in Advanced Non-small Cell Lung Cancer With Translational Research. U.S. National Institutes of Health. | ||||
Ref 525024 | ClinicalTrials.gov (NCT02314819) A Phase III Trial Evaluating Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer Patients ???RESCO). U.S. National Institutes of Health. | ||||
Ref 528395 | Ranibizumab: Phase III clinical trial results. Ophthalmol Clin North Am. 2006 Sep;19(3):361-72. | ||||
Ref 532104 | Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706. | ||||
Ref 541221 | (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: 5936). | ||||
Ref 541307 | (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: 6058). | ||||
Ref 541859 | (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: 6779). | ||||
Ref 542632 | (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: 7649). | ||||
Ref 542811 | (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: 7886). | ||||
Ref 542989 | (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: 8189). | ||||
Ref 546650 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009459) | ||||
Ref 548347 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024862) | ||||
Ref 525382 | E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. | ||||
Ref 526484 | J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. | ||||
Ref 526575 | J 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. | ||||
Ref 528467 | Development of ranibizumab, an anti-vascular endothelial growth factor antigen binding fragment, as therapy for neovascular age-related macular degeneration. Retina. 2006 Oct;26(8):859-70. | ||||
Ref 532104 | Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706. | ||||
Ref 532445 | Icrucumab, a fully human monoclonal antibody against the vascular endothelial growth factor receptor-1, in the treatment of patients with advanced solid malignancies: a Phase 1 study. Invest New Drugs. 2014 Apr;32(2):303-11. | ||||
Ref 533061 | Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45. | ||||
Ref 541307 | (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: 6058). |
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