Multiple kinases including BRAF, CRAF, VEGFR2, VEGFR3, PDGFR-β, FLT3, KIT, RET

The entry "Multiple kinases including BRAF, CRAF, VEGFR2, VEGFR3, PDGFR-β, FLT3, KIT, RET" covers a group of structurally and functionally related kinases that are central regulators of cell growth, survival, angiogenesis, and differentiation. These targets are either serine/threonine kinases (BRAF, CRAF/RAF1) or receptor tyrosine kinases (VEGFR2, VEGFR3, PDGFR-β, FLT3, KIT, RET). Mutations or dysregulation in these kinases are common in many cancers (such as melanoma, renal cell carcinoma, gastrointestinal stromal tumors, thyroid cancers, and some leukemias), making them prime therapeutic targets. Drugs that inhibit several of these kinases simultaneously (multikinase inhibitors) are broadly used in oncology and have demonstrated clinical benefit, but present significant safety challenges due to their broad activity spectrum.

Other names

multikinase targetsB-Rafv-Raf murine sarcoma viral oncogene homolog B1RAF1c-RafKDRFLK-1FLT4Platelet-derived growth factor receptor betaFms-like tyrosine kinase 3c-KitCD117Proto-oncogene tyrosine-protein kinase Ret

Inhibition of kinase activity by ATP-competitive binding, leading to blockade of downstream signaling pathways (MAPK, PI3K/Akt, PLCγ, etc.), ultimately resulting in decreased cell proliferation, angiogenesis, and survival.