Vascular endothelial growth factor receptor tyrosine kinase (VEGFR)

Vascular endothelial growth factor receptor tyrosine kinases (VEGFRs) are a family of cell-surface receptor tyrosine kinases that serve as the primary signal transducers for the vascular endothelial growth factor (VEGF) family of ligands[1][3][4][6]. There are three main human subtypes: VEGFR-1 (FLT1), VEGFR-2 (KDR/Flk-1), and VEGFR-3 (FLT4); each plays a critical role in mediating angiogenesis, vasculogenesis, and the maintenance of endothelial cell function[1][3]. Upon ligand binding, these receptors dimerize, autophosphorylate, and activate multiple intracellular signaling cascades that regulate vascular permeability, endothelial cell proliferation, migration, and survival[1][3]. VEGFRs are prominently involved in tumor-induced angiogenesis and are validated therapeutic targets in numerous cancers and other diseases marked by pathological blood vessel formation. Numerous small-molecule tyrosine kinase inhibitors and monoclonal antibodies targeting this pathway are approved for clinical use, though challenges remain due to potential toxicities and the development of drug resistance[1][7].

Other names

Vascular endothelial growth factor receptor (VEGFR)FMS-like tyrosine kinase (FLT)fms related receptor tyrosine kinase (FLT1, FLT4, KDR)VEGFR-1 (FLT1)VEGFR-2 (KDR/Flk-1)VEGFR-3 (FLT4)Fms related tyrosine kinase 1KDR (kinase insert domain receptor)Flk-1

Inhibition of receptor tyrosine kinase autophosphorylation; Blockade of VEGF-induced signaling; Suppression of angiogenesis and neovascularization