Target Information
| Target General Information | Top | |||||
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| Target ID |
T20761
(Former ID: TTDNS00542)
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| Target Name |
Vascular endothelial growth factor A (VEGFA)
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| Synonyms |
Vascular permeability factor; VPF; VEGF-A; VEGF
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| Gene Name |
VEGFA
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Colorectal cancer [ICD-11: 2B91] | |||||
| 2 | Retinopathy [ICD-11: 9B71] | |||||
| 3 | Vascular system developmental anomaly [ICD-11: LA90] | |||||
| Function |
Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of blood vessels. Binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activate downstream signaling pathways, does not activate angiogenesis and inhibits tumor growth. Binding to NRP1 receptor initiates a signaling pathway needed for motor neuron axon guidance and cell body migration, including for the caudal migration of facial motor neurons from rhombomere 4 to rhombomere 6 during embryonic development. Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth.
Click to Show/Hide
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| BioChemical Class |
Growth factor
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| UniProt ID | ||||||
| Sequence |
MNFLLSWVHWSLALLLYLHHAKWSQAAPMAEGGGQNHHEVVKFMDVYQRSYCHPIETLVD
IFQEYPDEIEYIFKPSCVPLMRCGGCCNDEGLECVPTEESNITMQIMRIKPHQGQHIGEM SFLQHNKCECRPKKDRARQEKKSVRGKGKGQKRKRKKSRYKSWSVYVGARCCLMPWSLPG PHPCGPCSERRKHLFVQDPQTCKCSCKNTDSRCKARQLELNERTCRCDKPRR Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A01487 | |||||
| HIT2.0 ID | T42EAZ | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Aflibercept | Drug Info | Approved | Metastatic colorectal cancer | [1] | |
| 2 | Bevacizumab | Drug Info | Approved | Metastatic colorectal cancer | [2] | |
| 3 | Brolucizumab | Drug Info | Approved | Wet age-related macular degeneration | [3] | |
| 4 | Ranibizumab | Drug Info | Approved | Hereditary hemorrhagic telangiectasia | [4], [5] | |
| Clinical Trial Drug(s) | [+] 16 Clinical Trial Drugs | + | ||||
| 1 | Avastin+/-Tarceva | Drug Info | Phase 3 | Non-small-cell lung cancer | [6] | |
| 2 | Bevacizumab + Erlotinib | Drug Info | Phase 3 | Metastatic colorectal cancer | [7], [8] | |
| 3 | Bevacizumab + Rituximab | Drug Info | Phase 3 | Non-hodgkin lymphoma | [9] | |
| 4 | Bevacizumab + Trastuzumab | Drug Info | Phase 3 | Breast cancer | [10] | |
| 5 | Faricimab | Drug Info | Phase 3 | Diabetic macular edema | [11] | |
| 6 | Abicipar pegol | Drug Info | Phase 2 | Diabetic macular edema | [12] | |
| 7 | PTC299 | Drug Info | Phase 2 | Rheumatoid arthritis | [13], [14] | |
| 8 | RG7221 | Drug Info | Phase 2 | Colorectal cancer | [15] | |
| 9 | RO5520985 | Drug Info | Phase 2 | Colorectal cancer | [16] | |
| 10 | MP0250 | Drug Info | Phase 1/2 | Non-small-cell lung cancer | [17] | |
| 11 | SNN-0029 | Drug Info | Phase 1/2 | Lateral sclerosis | [18] | |
| 12 | ABI-011 | Drug Info | Phase 1 | Solid tumour/cancer | [19] | |
| 13 | AT001/r84 | Drug Info | Phase 1 | Solid tumour/cancer | [20] | |
| 14 | MP-0112 | Drug Info | Phase 1 | Macular degeneration | [21] | |
| 15 | Navicixizumab | Drug Info | Phase 1 | Colorectal cancer | [22] | |
| 16 | SFLT-01 | Drug Info | Phase 1 | Macular degeneration | [23] | |
| Patented Agent(s) | [+] 13 Patented Agents | + | ||||
| 1 | 3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivative 1 | Drug Info | Patented | Cell proliferative disorder | [24] | |
| 2 | Antibodie derivative 7 | Drug Info | Patented | Solid tumour/cancer | [24] | |
| 3 | Antibodie derivative 9 | Drug Info | Patented | Corneal neovascularization | [24] | |
| 4 | Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 | Drug Info | Patented | Gastric adenocarcinoma | [24] | |
| 5 | Oxetane 3,3-dicarboxamide compound 1 | Drug Info | Patented | Virus infection | [24] | |
| 6 | Oxetane 3,3-dicarboxamide compound 2 | Drug Info | Patented | Virus infection | [24] | |
| 7 | PMID28621580-Compound-WO2013036866C66 | Drug Info | Patented | Solid tumour/cancer | [24] | |
| 8 | PMID28621580-Compound-WO2013112959C68 | Drug Info | Patented | Fibrosis | [24] | |
| 9 | PMID28621580-Compound-WO2015089220C70 | Drug Info | Patented | Retinopathy | [24] | |
| 10 | Pyridine derivative 4 | Drug Info | Patented | Solid tumour/cancer | [24] | |
| 11 | Pyrimidine derivative 5 | Drug Info | Patented | Neurodegenerative disorder | [24], [25], [26] | |
| 12 | Pyrimidine derivative 6 | Drug Info | Patented | Neurodegenerative disorder | [24], [25], [26] | |
| 13 | Pyrimidine derivative 7 | Drug Info | Patented | Neurodegenerative disorder | [24], [25], [26] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | Bevasiranib | Drug Info | Discontinued in Phase 3 | Exudative age-related macular degeneration | [27] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Modulator | [+] 7 Modulator drugs | + | ||||
| 1 | Aflibercept | Drug Info | [1] | |||
| 2 | PTC299 | Drug Info | [33] | |||
| 3 | RG7221 | Drug Info | [34] | |||
| 4 | RO5520985 | Drug Info | [35] | |||
| 5 | SNN-0029 | Drug Info | [36] | |||
| 6 | SFLT-01 | Drug Info | [38] | |||
| 7 | Bevasiranib | Drug Info | [39] | |||
| Inhibitor | [+] 66 Inhibitor drugs | + | ||||
| 1 | Bevacizumab | Drug Info | [2] | |||
| 2 | Brolucizumab | Drug Info | [3] | |||
| 3 | Avastin+/-Tarceva | Drug Info | [29], [30] | |||
| 4 | Bevacizumab + Erlotinib | Drug Info | [31] | |||
| 5 | Bevacizumab + Rituximab | Drug Info | [31] | |||
| 6 | Bevacizumab + Trastuzumab | Drug Info | [31] | |||
| 7 | Abicipar pegol | Drug Info | [12] | |||
| 8 | MP0250 | Drug Info | [17] | |||
| 9 | ABI-011 | Drug Info | [17] | |||
| 10 | MP-0112 | Drug Info | [37] | |||
| 11 | 1,6-naphyridine-4-ketone fused heterocyclic derivative 1 | Drug Info | [24] | |||
| 12 | 3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivative 1 | Drug Info | [24] | |||
| 13 | Antibodie derivative 4 | Drug Info | [24] | |||
| 14 | Carbamide derivative 14 | Drug Info | [24] | |||
| 15 | Carbamide derivative 15 | Drug Info | [24] | |||
| 16 | Carbamide derivative 16 | Drug Info | [24] | |||
| 17 | Carbamide derivative 17 | Drug Info | [24] | |||
| 18 | Carbamide derivative 18 | Drug Info | [24] | |||
| 19 | Carbamide derivative 19 | Drug Info | [24] | |||
| 20 | Carbamide derivative 20 | Drug Info | [24] | |||
| 21 | Carbamide derivative 21 | Drug Info | [24] | |||
| 22 | Carbamide derivative 22 | Drug Info | [24] | |||
| 23 | Carbamide derivative 23 | Drug Info | [24] | |||
| 24 | Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 | Drug Info | [24] | |||
| 25 | Indoline derivative 12 | Drug Info | [24] | |||
| 26 | Indoline derivative 13 | Drug Info | [24] | |||
| 27 | Indoline derivative 14 | Drug Info | [24] | |||
| 28 | Indoline derivative 15 | Drug Info | [24] | |||
| 29 | Indoline derivative 16 | Drug Info | [24] | |||
| 30 | Indoline derivative 17 | Drug Info | [24] | |||
| 31 | Indoline derivative 18 | Drug Info | [24] | |||
| 32 | Indoline derivative 19 | Drug Info | [24] | |||
| 33 | Indoline derivative 20 | Drug Info | [24] | |||
| 34 | Indoline derivative 21 | Drug Info | [24] | |||
| 35 | Oxetane 3,3-dicarboxamide compound 1 | Drug Info | [24] | |||
| 36 | Oxetane 3,3-dicarboxamide compound 2 | Drug Info | [24] | |||
| 37 | PMID28621580-Compound-WO2013036866C66 | Drug Info | [24] | |||
| 38 | PMID28621580-Compound-WO2013112959C68 | Drug Info | [24] | |||
| 39 | PMID28621580-Compound-WO2014079545C69 | Drug Info | [24] | |||
| 40 | PMID28621580-Compound-WO2015089220C70 | Drug Info | [24] | |||
| 41 | Pyridine derivative 10 | Drug Info | [24] | |||
| 42 | Pyridine derivative 11 | Drug Info | [24] | |||
| 43 | Pyridine derivative 2 | Drug Info | [24] | |||
| 44 | Pyridine derivative 3 | Drug Info | [24] | |||
| 45 | Pyridine derivative 4 | Drug Info | [24] | |||
| 46 | Pyridine derivative 5 | Drug Info | [24] | |||
| 47 | Pyridine derivative 6 | Drug Info | [24] | |||
| 48 | Pyridine derivative 7 | Drug Info | [24] | |||
| 49 | Pyridine derivative 8 | Drug Info | [24] | |||
| 50 | Pyridine derivative 9 | Drug Info | [24] | |||
| 51 | Pyrimidine derivative 10 | Drug Info | [24] | |||
| 52 | Pyrimidine derivative 11 | Drug Info | [24] | |||
| 53 | Pyrimidine derivative 5 | Drug Info | [24] | |||
| 54 | Pyrimidine derivative 6 | Drug Info | [24] | |||
| 55 | Pyrimidine derivative 7 | Drug Info | [24] | |||
| 56 | Pyrimidine derivative 8 | Drug Info | [24] | |||
| 57 | Pyrimidine derivative 9 | Drug Info | [24] | |||
| 58 | Quinoline and quinazoline derivative 10 | Drug Info | [24] | |||
| 59 | Quinoline and quinazoline derivative 2 | Drug Info | [24] | |||
| 60 | Quinoline and quinazoline derivative 3 | Drug Info | [24] | |||
| 61 | Quinoline and quinazoline derivative 4 | Drug Info | [24] | |||
| 62 | Quinoline and quinazoline derivative 5 | Drug Info | [24] | |||
| 63 | Quinoline and quinazoline derivative 6 | Drug Info | [24] | |||
| 64 | Quinoline and quinazoline derivative 7 | Drug Info | [24] | |||
| 65 | Quinoline and quinazoline derivative 8 | Drug Info | [24] | |||
| 66 | Quinoline and quinazoline derivative 9 | Drug Info | [24] | |||
| Blocker | [+] 1 Blocker drugs | + | ||||
| 1 | Antibodie derivative 1 | Drug Info | [24] | |||
| Binder | [+] 2 Binder drugs | + | ||||
| 1 | Antibodie derivative 2 | Drug Info | [24] | |||
| 2 | Antibodie derivative 7 | Drug Info | [24] | |||
| Disrupter | [+] 1 Disrupter drugs | + | ||||
| 1 | Antibodie derivative 8 | Drug Info | [24] | |||
| Stablizer | [+] 1 Stablizer drugs | + | ||||
| 1 | Antibodie derivative 9 | Drug Info | [24] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2004. Application Number: (ANDA) 125085. | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019 | |||||
| REF 4 | URL: 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 5 | Ranibizumab: Phase III clinical trial results. Ophthalmol Clin North Am. 2006 Sep;19(3):361-72. | |||||
| REF 6 | Clinical pipeline report, company report or official report of Roche. | |||||
| REF 7 | ClinicalTrials.gov (NCT00130728) A Study to Evaluate the Efficacy of Bevacizumab in Combination With Tarceva for Advanced Non-Small Cell Lung Cancer | |||||
| REF 8 | ClinicalTrials.gov (NCT00598156) Chemotherapy and Avastin Followed by Maintenance Treatment With Avastin +/- Tarceva | |||||
| REF 9 | ClinicalTrials.gov (NCT00486759) A Study of Bevacizumab (Avastin) in Combination With Rituximab (MabThera) and CHOP (Cyclophosphamide, Hydroxydaunorubicin [Doxorubicin], Oncovin [Vincristine], Prednisone) Chemotherapy in Patients With Diffuse Large B-cell Lymphoma. U.S. National Institutes of Health. | |||||
| REF 10 | AVEREL: a randomized phase III Trial evaluating bevacizumab in combination with docetaxel and trastuzumab as first-line therapy for HER2-positive locally recurrent/metastatic breast cancer. J Clin Oncol. 2013 May 10;31(14):1719-25. | |||||
| REF 11 | ClinicalTrials.gov (NCT04432831) A Study to Evaluate the Long-Term Safety and Tolerability of Faricimab in Participants With Diabetic Macular Edema (Rhone-X). U.S. National Institutes of Health. | |||||
| REF 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 13 | URL: 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: 6040). | |||||
| REF 14 | The effects of antiinflammatory and antiallergic drugs on cytokine release after stimulation of human whole blood by lipopolysaccharide and zymosan A. Inflamm Res. 1995 Jul;44(7):269-74. | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037469) | |||||
| REF 16 | ClinicalTrials.gov (NCT02141295) A Study Comparing the Efficacy and Safety of Vanucizumab and FOLFOX With Bevacizumab and FOLFOX in Participants With Untreated Metastatic Colorectal Cancer | |||||
| REF 17 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 18 | ClinicalTrials.gov (NCT01384162) An Open Label, Safety and Tolerability Continuation Study of Intracerebroventricular Administration of sNN0029 to Patients With Amyotrophic Lateral Sclerosis. U.S. National Institutes of Health. | |||||
| REF 19 | ClinicalTrials.gov (NCT01163071) A Phase 1 Trial of ABI-011 in Patients With Advanced Solid Tumors or Lymphomas. U.S. National Institutes of Health. | |||||
| REF 20 | Clinical pipeline report, company report or official report of Affitech (2011). | |||||
| REF 21 | ClinicalTrials.gov (NCT01042678) Study of MP0112 Intravitreal Injection in Patients With Diabetic Macular Edema. U.S. National Institutes of Health. | |||||
| REF 22 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 23 | ClinicalTrials.gov (NCT01024998) Safety and Tolerability Study of AAV2-sFLT01 in Patients With Neovascular Age-Related Macular Degeneration (AMD). U.S. National Institutes of Health. | |||||
| REF 24 | VEGFR-2 inhibitors and the therapeutic applications thereof: a patent review (2012-2016).Expert Opin Ther Pat. 2017 Sep;27(9):987-1004. | |||||
| REF 25 | Novel NF-B inhibitors: a patent review (2011 - 2014).Expert Opin Ther Pat. 2015 Mar;25(3):319-34. | |||||
| REF 26 | Caspase inhibitors: a review of recently patented compounds (2013-2015).Expert Opin Ther Pat. 2018 Jan;28(1):47-59. | |||||
| REF 27 | 2011 Pipeline of Acuity Pharmaceuticals. | |||||
| REF 28 | 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 29 | Clinical pipeline report, company report or official report of Genentech (2009). | |||||
| REF 30 | Clinical pipeline report, company report or official report of Genentech (2009). | |||||
| REF 31 | Clinical pipeline report, company report or official report of Roche (2009). | |||||
| REF 32 | Faricimab: an investigational agent targeting the Tie-2/angiopoietin pathway and VEGF-A for the treatment of retinal diseases. Expert Opin Investig Drugs. 2021 Mar;30(3):193-200. | |||||
| REF 33 | Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study.J Neurooncol.2015 Jan;121(1):217-24. | |||||
| REF 34 | Bispecific antibodies and their applications | |||||
| REF 35 | Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. | |||||
| REF 36 | Clinical pipeline report, company report or official report of Neuronova. | |||||
| REF 37 | Treatment of exudative age-related macular degeneration with a designed ankyrin repeat protein that binds vascular endothelial growth factor: a phase I/II study. Am J Ophthalmol. 2014 Oct;158(4):724-732.e2. | |||||
| REF 38 | sFLT01: a novel fusion protein with antiangiogenic activity. Mol Cancer Ther. 2011 Mar;10(3):404-15. | |||||
| REF 39 | Bevasiranib for the Treatment of Wet, Age-Related Macular Degeneration | |||||
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