VEGFR-2, FGFR-1, FGFR-2

Vascular endothelial growth factor receptor 2 (VEGFR-2), fibroblast growth factor receptor 1 (FGFR-1), and fibroblast growth factor receptor 2 (FGFR-2) are single-pass transmembrane receptor tyrosine kinases expressed on the surface of various cell types. VEGFR-2 is the principal mediator of VEGF-driven angiogenesis, playing a central role in vascular development and pathological neovascularization such as tumor angiogenesis[4][3]. FGFR-1 and FGFR-2 are primary mediators of signaling by fibroblast growth factors, regulating critical processes including cell proliferation, differentiation, survival, embryonic development, and tissue repair[1][5].\nAberrant activation, overexpression, or mutation of these receptors is implicated in cancers and developmental diseases. As such, they are important therapeutic targets, with multiple approved and investigational drugs developed to inhibit their kinase activity and downstream signaling[2][6][8].

Other names

KDRFlk-1CD331CD332

Inhibition of tyrosine kinase activity: Most drugs competitively inhibit ATP binding to the receptor kinase domain, thus blocking downstream signaling vital for angiogenesis and cell growth.\nAntibody-mediated ligand/receptor blockade: Some act by preventing ligand binding or receptor dimerization.