Vascular endothelial growth factor receptor 2; Vascular endothelial growth factor receptor 3 (VEGFR-2 (also known as KDR/Flk-1); VEGFR-3 (also known as FLT4))

Vascular endothelial growth factor receptor 2 (VEGFR-2) and vascular endothelial growth factor receptor 3 (VEGFR-3) are cell surface receptor tyrosine kinases primarily expressed on vascular and lymphatic endothelial cells, respectively. VEGFR-2 is the principal mediator of VEGF-driven angiogenesis, promoting endothelial cell proliferation, migration, survival, and enhanced vascular permeability, crucial for both physiological and pathological blood vessel formation[4][5][7]. VEGFR-3, in contrast, mainly mediates lymphangiogenesis in response to VEGF-C and VEGF-D and is crucial in developmental and pathological lymphatic growth, with roles in tumor metastasis and lymphatic disorders[1][4][7]. Both receptors share a similar structure: an extracellular region with seven immunoglobulin-like domains, a single-pass transmembrane segment, and an intracellular split tyrosine kinase domain[3][4][5]. They are extensively targeted in oncology and ophthalmology for anti-angiogenic therapies, as well as being studied for potential therapies in lymphedema and lymphatic metastasis[7][8].

Other names

KDRFlk-1CD309FLT4Fms-like tyrosine kinase 4

Inhibition of ligand binding and subsequent receptor dimerization Inhibition of tyrosine kinase activity, blocking downstream signaling (such as PI3K/AKT and MAPK/ERK pathways)