RAF, VEGFR, PDGFR kinases (RAF, VEGFR, PDGFR)

RAF, VEGFR, and PDGFR kinases are protein kinases essential for intracellular signaling related to cell proliferation, survival, and migration. RAF kinases act downstream of RAS to activate the MEK-ERK pathway, influencing cell division and cancer growth[3]. VEGFR kinases, especially VEGFR-2, regulate angiogenesis and vasculogenesis by mediating the effects of vascular endothelial growth factors on endothelial cell growth, survival, and permeability[1][2]. PDGFR kinases are critical for embryonic development, tissue repair, and the regulation of cell proliferation by binding platelet-derived growth factors[5][6]. All three are frequently targeted in cancer therapy, as their dysregulation is implicated in tumor formation, progression, and resistance to therapy. Drugs inhibiting these kinases are approved for various cancers, but notable safety concerns exist due to their roles in normal tissue function.

Other names

RAFRaf-1c-RafARAFBRAFVEGFRKDR (human VEGFR-2)Flk-1 (mouse VEGFR-2)Flt-1 (VEGFR-1)PDGFRPDGFRαPDGFRβ

Competitive inhibition of ATP binding to the kinase domain; Blockade of downstream signaling (MAPK/ERK pathway for RAF; angiogenesis pathways for VEGFR and PDGFR); Induction of cell cycle arrest and apoptosis by disrupt signaling