VEGFA   

GtoPdb Ligand ID: 5085

Synonyms: vascular endothelial growth factor A | vascular permeability factor (VPF) | VEGF-A
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 [13-14].
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
Natural/Endogenous Targets
Target
fms related receptor tyrosine kinase 1
kinase insert domain receptor
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
kinase insert domain receptor Hs Agonist Agonist 8.0 – 9.6 pKd - 10
pKd 9.6 (Kd 2.3x10-10 M) [10]
Description: Dissociation constant for scVEGF-binding to dimeric VEGFR2.
pKd 8.0 (Kd 1x10-8 M) [10]
Description: Dissociation constant for scVEGF-binding to monomeric VEGFR2.
fms related receptor tyrosine kinase 1 Hs None - - - -
kinase insert domain receptor Hs None - - - -
Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
abicipar pegol Hs Inhibitor Inhibition 11.7 pKd - 6
pKd 11.7 (Kd 2x10-12 M) [6]
vanucizumab Hs Antibody Binding >10.0 pKd - 4
pKd >10.0 (Kd <1x10-10 M) [4]
ranibizumab Hs Antibody Binding 9.8 pKd - 2
pKd 9.8 (Kd 1.5x10-10 M) [2]
brolucizumab Hs Antibody Binding 8.8 pKd - 5
pKd 8.8 (Kd 1.59x10-9 M) [5]
bevacizumab Hs Antibody Binding 8.0 – 8.3 pIC50 - 2
pIC50 8.0 – 8.3 (IC50 1x10-8 – 5x10-9 M) [2]
aflibercept Hs Antagonist Inhibition - - - 7-8,12
[7-8,12]
pegaptanib Hs Antagonist Inhibition - - - 9,11
[9,11]
Ligand mentioned in the following text fields