VEGFR1, VEGFR2, VEGFR3, PDGFRα, PDGFRβ, KIT Target List (VEGFR1, VEGFR2, VEGFR3, PDGFRα, PDGFRβ, KIT)

This target group encompasses the vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), the platelet-derived growth factor receptors (PDGFRα and PDGFRβ), and mast/stem cell growth factor receptor Kit. All are class III receptor tyrosine kinases with similar domain architecture (five to seven immunoglobulin-like domains extracellularly, single transmembrane span, intracellular split kinase domain), and regulate diverse cellular processes including angiogenesis, lymphangiogenesis, cell proliferation, survival, and migration. They play central roles in both normal physiology (such as vascular and hematopoietic development) and in pathologies including cancer, where aberrant signaling supports tumor growth, metastasis, and resistance to therapy. Multi-kinase inhibitors targeting various combinations of these receptors are approved for several cancer indications and are under active development for additional therapeutic uses.

Other names

Flt-1 (VEGFR1)KDR (VEGFR2, human) / Flk-1 (VEGFR2, murine)Flt-4 (VEGFR3)CD117 (KIT)c-Kit (KIT)PDGFR-A, PDGFR-alpha (PDGFRα)PDGFR-B, PDGFR-beta (PDGFRβ)

Small molecule tyrosine kinase inhibition (most interacting drugs block the ATP-binding pocket); Blockade of ligand-induced receptor dimerization and autophosphorylation; Downregulation of downstream signaling pathways (e.g., MAPK, PI3K/AKT).