Vascular endothelial growth factor A receptor pathway (VEGFR (for the family; specific subtypes are VEGFR-1, VEGFR-2))

The vascular endothelial growth factor A receptor, commonly referred to as VEGF receptor, is a family of cell surface tyrosine kinase receptors that mediate cellular responses to vascular endothelial growth factors. The main subtypes relevant for VEGF-A signaling are VEGFR‑1 (Flt‑1) and VEGFR‑2 (KDR/Flk‑1). Upon binding their ligand—primarily VEGF-A—these receptors dimerize and autophosphorylate their intracellular domains, initiating multiple downstream signaling cascades that regulate angiogenesis, vasculogenesis, vascular permeability, cell survival/proliferation/migration in endothelium. This pathway is essential during embryonic development but also plays a central role in pathological conditions such as tumor neovascularization. Therapeutic targeting focuses on blocking either ligand-receptor interaction or inhibiting intracellular kinase activity using monoclonal antibodies or small molecule inhibitors.

Other names

Vascular endothelial growth factor receptorVEGF receptorFlt-1 (VEGFR-1)KDR/Flk-1 (VEGFR-2)

Drugs act by: - Inhibiting ligand binding to the receptor (e.g., monoclonal antibodies like bevacizumab block VEGF-A from binding to its receptors) - Inhibiting tyrosine kinase activity of the receptors or downstream signaling pathways such as RAS/RAF/MEK/ERK and PI3K/AKT/mTOR cascades with small molecule inhibitors