VEGFR2, FGFR1, PDGFRα, and KIT (VEGFR2, FGFR1, PDGFRα, KIT)

These four proteins—vascular endothelial growth factor receptor 2, fibroblast growth factor receptor 1, platelet-derived growth factor receptor alpha, and mast/stem cell growth factor receptor Kit—are cell-surface receptor tyrosine kinases that mediate essential signaling pathways for cell proliferation, differentiation, survival, migration, and angiogenesis. Dysregulation or overexpression of these targets is implicated in cancer progression, neovascularization, and other diseases, making them important targets for multi-tyrosine kinase inhibitors. Drugs targeting these receptors are approved and in clinical trials for a range of malignancies and other pathologies. Their signaling is primarily controlled by growth factor binding, dimerization, and activation of intracellular kinase domains, resulting in phosphorylation events that stimulate cellular responses relevant to disease and therapy.

Other names

KDRFlk-1FGFR-1PDGFR-alphaPDGFRAc-KitCD117

Tyrosine kinase inhibition: Drugs typically inhibit the ATP-binding site of the intracellular kinase domain, blocking receptor auto-phosphorylation and downstream signaling. Anti-angiogenic effect: Inhibition of angiogenesis, proliferation, survival, and migration pathways, mostly through suppression of VEGF-VEGFR2 and FGF-FGFR1 signaling. Induction of apoptosis and suppression of cell growth.