VEGFR

VEGFR inhibitors act on the receptor tyrosine kinases activated by vascular endothelial growth factor (VEGF). Three VEGF receptors (VEGFRs) regulate the growth of blood and lymphatic vessels. VEGFR2, also known as kinase insert domain receptor (KDR) or Flk-1, mediates most endothelial responses to VEGF-A, and VEGFR3 mainly controls lymphatic vessels. Mice lacking Flk-1 fail to form blood islands and blood vessels, which shows the central role of this receptor in vasculogenesis. Most compounds here bind the kinase domain and also inhibit related receptors such as the platelet-derived growth factor receptor (PDGFR) and c-Kit. Axitinib and SU 5416 (semaxinib) are used as VEGFR-focused tools, while lenvatinib and regorafenib cover broader kinase sets.

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