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Synonyms: vascular endothelial growth factor A | vascular permeability factor (VPF) | VEGF-A
Compound class:
Endogenous peptide in human, mouse or rat
Comment: The active peptide is anti-parallel homodimer linked by disulphide bonds. VEGFA exists as four isoforms of 121, 165, 189 and 206 amino acids. The shortest variant contains the full VEGFR2 binding site but lacks domains that are involved in interactions with extracellular-matrix and co-receptors which are present in the longer isoforms [14-15].
A recombinant single-chain derivative of VEGFA121 (scVEGF) can be used experimentally as a fully functional peptide that binds and activates VEGFR2 in the same manner as endogenous VEGFA [1]. scVEGF can be labelled with a single fluorophore at its N-terminal, for use as a molecular probe [3].
Species: Human
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Anderson CR, Rychak JJ, Backer M, Backer J, Ley K, Klibanov AL. (2010)
scVEGF microbubble ultrasound contrast agents: a novel probe for ultrasound molecular imaging of tumor angiogenesis. Invest Radiol, 45 (10): 579-85. [PMID:20733505] |
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2. Baca M, Chen Y M-Y, Lowman HB, Presta LG, Wells JA. (1998)
Anti-vegf antibodies. Patent number: WO1998045331. Assignee: Genentech Inc,. Priority date: 07/04/1997. Publication date: 15/10/1998. |
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3. Backer MV, Backer JM. (2001)
Targeting endothelial cells overexpressing VEGFR-2: selective toxicity of Shiga-like toxin-VEGF fusion proteins. Bioconjug Chem, 12 (6): 1066-73. [PMID:11716701] |
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4. Baehner M, Imhof-Jung S, Kavlie A, Kettenberger H, Klein C, Thomas J, Schaefer W, Stubenrauch K-G, Thomas M. (2015)
Bispecific, bivalent anti-VEGF/anti-ANG-2 antibodies. Patent number: US8945552 B2. Assignee: Hoffmann-La Roche Inc.. Priority date: 26/03/2010. Publication date: 03/02/2015. |
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5. Borras L, Urech D, Gunde T. (2013)
Stable and soluble antibodies inhibiting VEGF. Patent number: US8349322 B2. Assignee: ESBATech, an Alcon Biomedical Research Unit, LLC.. Priority date: 25/06/2008. Publication date: 08/01/2013. |
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6. Campochiaro PA, Channa R, Berger BB, Heier JS, Brown DM, Fiedler U, Hepp J, Stumpp MT. (2013)
Treatment of diabetic macular edema with a designed ankyrin repeat protein that binds vascular endothelial growth factor: a phase I/II study. Am J Ophthalmol, 155 (4): 697-704, 704.e1-2. [PMID:23218689] |
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7. Chang AA, Li H, Broadhead GK, Hong T, Schlub TE, Wijeyakumar W, Zhu M. (2014)
Intravitreal aflibercept for treatment-resistant neovascular age-related macular degeneration. Ophthalmology, 121 (1): 188-92. [PMID:24144450] |
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8. Chu QS. (2009)
Aflibercept (AVE0005): an alternative strategy for inhibiting tumour angiogenesis by vascular endothelial growth factors. Expert Opin Biol Ther, 9 (2): 263-71. [PMID:19236257] |
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9. Gragoudas ES, Adamis AP, Cunningham Jr ET, Feinsod M, Guyer DR, VEGF Inhibition Study in Ocular Neovascularization Clinical Trial Group. (2004)
Pegaptanib for neovascular age-related macular degeneration. N Engl J Med, 351 (27): 2805-16. [PMID:15625332] |
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10. King C, Hristova K. (2019)
Direct measurements of VEGF-VEGFR2 binding affinities reveal the coupling between ligand binding and receptor dimerization. J Biol Chem, 294 (23): 9064-9075. [PMID:31023826] |
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11. Nimjee SM, Rusconi CP, Sullenger BA. (2005)
Aptamers: an emerging class of therapeutics. Annu Rev Med, 56: 555-83. [PMID:15660527] |
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12. Regula JT, Lundh von Leithner P, Foxton R, Barathi VA, Cheung CM, Bo Tun SB, Wey YS, Iwata D, Dostalek M, Moelleken J et al.. (2016)
Targeting key angiogenic pathways with a bispecific CrossMAb optimized for neovascular eye diseases. EMBO Mol Med, 8 (11): 1265-1288. [PMID:27742718] |
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13. Tang PA, Moore MJ. (2013)
Aflibercept in the treatment of patients with metastatic colorectal cancer: latest findings and interpretations. Therap Adv Gastroenterol, 6 (6): 459-73. [PMID:24179482] |
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14. Vempati P, Popel AS, Mac Gabhann F. (2014)
Extracellular regulation of VEGF: isoforms, proteolysis, and vascular patterning. Cytokine Growth Factor Rev, 25 (1): 1-19. [PMID:24332926] |
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15. Zachary IC. (2011)
How neuropilin-1 regulates receptor tyrosine kinase signalling: the knowns and known unknowns. Biochem Soc Trans, 39 (6): 1583-91. [PMID:22103491] |
