Vascular endothelial growth factor receptor 2 (VEGFR-2)

Vascular endothelial growth factor receptor 2 (VEGFR-2) is a transmembrane receptor tyrosine kinase that plays a central role in mediating the effects of vascular endothelial growth factor A (VEGF-A) as well as other VEGF family ligands. It consists of an extracellular domain with seven immunoglobulin-like subdomains (forming the primary VEGF-A binding site), a single transmembrane helix, and an intracellular tyrosine kinase domain that becomes activated upon ligand-induced receptor dimerization and autophosphorylation. Activation of VEGFR-2 initiates multiple intracellular signaling cascades that are critical for endothelial cell proliferation, survival, migration, and vascular permeability, making it a key regulator of angiogenesis and vasculogenesis both in physiological and pathological processes. Overactivation of VEGFR-2 signaling is implicated in tumor growth, metastasis, and a variety of diseases linked to abnormal vessel formation. Multiple targeted therapies inhibit VEGFR-2 directly or block its ligands to disrupt pathological angiogenesis, particularly in cancer treatment. VEGFR-2 modulation can have significant side effects due to its importance in vascular function and homeostasis

Other names

VEGFR-2Kinase insert domain receptor (KDR)Fetal liver kinase 1 (Flk-1)Vascular endothelial growth factor receptor type 2

- Inhibition of VEGFR-2 kinase activity (by small molecules or antibodies) - Blockade of VEGF ligand binding to VEGFR-2 (by monoclonal antibodies or decoy receptors) - Downregulation of downstream signaling leading to reduced angiogenesis and tumor vascularization