Vascular endothelial growth factor receptor (VEGFR)

Vascular endothelial growth factor receptors (VEGFRs) are a family of receptor tyrosine kinases that bind vascular endothelial growth factors (VEGFs). There are three main subtypes: VEGFR-1 (FLT1), VEGFR-2 (KDR/Flk-1), and VEGFR-3 (Flt-4). Their extracellular regions consist of seven immunoglobulin-like domains, a single transmembrane helix, and a cytoplasmic split tyrosine kinase domain. Upon ligand binding, VEGFRs dimerize and undergo phosphorylation, initiating intracellular signaling pathways that regulate endothelial cell proliferation, migration, survival, and vascular permeability. VEGFRs play essential roles in blood vessel formation (angiogenesis, vasculogenesis) and lymphatic vessel formation (VEGFR-3). They are well-validated targets for anti-angiogenic cancer therapy as well as for other diseases involving pathological angiogenesis and vascular permeability. Several small molecule inhibitors and antibody drugs target VEGFRs or their ligands, but their use is associated with safety concerns, especially due to their role in normal vascular homeostasis

Other names

VEGFRVascular endothelial growth factor receptor 1VEGFR-1FLT1Vascular endothelial growth factor receptor 2VEGFR-2KDR/Flk-1Vascular endothelial growth factor receptor 3VEGFR-3Flt-4mbVEGFRsVEGFR

Inhibition of receptor tyrosine kinase activity (prevents autophosphorylation and downstream signaling); Ligand sequestration (antibody binds VEGF ligand, prevents receptor activation); Inhibition of angiogenesis and vascular permeability