Vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR-1, VEGFR-2, VEGFR-3)

Vascular endothelial growth factor receptors 1, 2, and 3 are cell surface receptor tyrosine kinases essential for angiogenesis, vasculogenesis, and lymphangiogenesis. Each receptor comprises an extracellular region with seven immunoglobulin-like domains, a single transmembrane region, and a cytoplasmic split kinase domain. VEGFR-1 primarily modulates VEGFR-2 signaling and can act as a decoy, binding VEGF-A and regulating vascular formation. VEGFR-2 is the principal mediator of VEGF-driven endothelial cell proliferation, migration, survival, and vascular permeability, serving as a major therapeutic target in oncology and ophthalmology. VEGFR-3 is mostly expressed in lymphatic endothelial cells and is crucial for the formation, migration, and survival of lymphatic vessels, with roles in embryonic vascular development and lymphatic disorders. Dysregulation of VEGFRs is implicated in cancers, cardiovascular disease, inflammatory conditions, and lymphatic pathologies, making all three receptors key therapeutic drug targets.

Other names

VEGFR-1: FLT-1VEGFR-2: KDRVEGFR-2: Flk-1VEGFR-3: FLT-4Tyrosine kinase receptor familyFetal liver kinase (VEGFR-2 in mouse)

Tyrosine kinase inhibition (most small molecules: sunitinib, sorafenib, etc.) Ligand sequestration (antibodies binding VEGF: bevacizumab) Preventing receptor dimerization and activation (monoclonal antibodies: ramucirumab)