Vascular endothelial growth factor receptor 2 (VEGFR2) (VEGFR2)

Vascular endothelial growth factor receptor 2 (VEGFR2) is a critical transmembrane receptor tyrosine kinase primarily expressed on vascular endothelial cells (UniProt: P35968). It serves as the principal mediator of the biological effects of VEGF-A, including the induction of angiogenesis, vasculogenesis, and increased vascular permeability (PubMed: 11046056). Upon binding to its ligands, VEGFR2 undergoes dimerization and autophosphorylation of its intracellular kinase domain, activating downstream signaling cascades such as the MAPK/ERK and PI3K/Akt pathways (StatPearls: NBK542235). In many pathological conditions, particularly solid tumors, VEGFR2 is overexpressed or overstimulated, facilitating the formation of new blood vessels that support tumor growth and metastasis (PubMed: 15322176). Therapeutic strategies targeting VEGFR2 include monoclonal antibodies like ramucirumab that block the extracellular binding site and small-molecule inhibitors like sunitinib that target the intracellular kinase activity (NIH: PMC3136665). While effective in slowing disease progression, these therapies are often associated with systemic side effects like hypertension and proteinuria due to the receptor's role in maintaining normal vascular homeostasis (PubMed: 19138116).

Other names

Kinase insert domain receptorKDRFetal liver kinase 1FLK1CD309Protein-tyrosine kinase receptor flk-1VEGF type-2 receptor

Inhibition of the intracellular tyrosine kinase domain or blockade of the extracellular ligand-binding domain to prevent VEGF-mediated signaling (StatPearls: NBK542235).