Vascular endothelial growth factor receptor 2, Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 2 (VEGFR2, FGFR1, FGFR2)

Vascular endothelial growth factor receptor 2 (VEGFR2), fibroblast growth factor receptor 1 (FGFR1), and fibroblast growth factor receptor 2 (FGFR2) are single-pass transmembrane receptor tyrosine kinases and members of the class III (VEGFR) and class IV (FGFR) receptor tyrosine kinase families, respectively[1][2][7]. VEGFR2 is primarily expressed on vascular endothelial cells and is the central signaling receptor for VEGF-A, making it an essential mediator of both normal and pathological angiogenesis[1][7]. FGFR1 and FGFR2 bind various FGFs and regulate diverse cellular processes, including cell proliferation, differentiation, survival, migration, tissue remodeling, and embryonic development[2][3][5][6]. Aberrations in these receptors, such as mutations, amplifications, or gene fusions, are implicated in cancer, developmental anomalies, and other human diseases[3][6]. Targeted therapies—including small-molecule kinase inhibitors—have been developed for clinical use, particularly in oncology, to block these signaling pathways and their role in tumor growth and angiogenesis[4][6][7].

Other names

KDRFlk-1CD331CD332Tyrosine-protein kinase receptorKinase insert domain receptor (VEGFR2)Fibroblast growth factor receptor 1Fibroblast growth factor receptor 2

Competitive inhibition of ATP binding at the kinase domain, blocking downstream signal transduction Inhibition of receptor autophosphorylation Inhibition of angiogenesis and tumor vascularization Suppression of cancer cell proliferation and survival