Tyrosine Kinase
Receptor tyrosine kinases bind to extracellular ligands/growth factors, which promotes receptor dimerization and autophosphorylation of receptor tyrosine residues. This triggers a cascade of downstream events through phosphorylation of intracellular proteins that ultimately transduce the extracellular signal to the nucleus, causing changes in gene expression. Receptor tyrosine kinases include EGFR/ErbB, PDGFR, VEGFR, FGFR and MET subfamilies etc. Dysfunctions in tyrosine phosphorylation are linked to oncogenic transformation. In additions, various adaptor and effector proteins couple to carboxy-terminal of an active kinase. For instance, binding of the GRB2 adaptor protein activates EGFR and MAPK/ERK signaling.
Non-receptor tyrosine kinases involve many well-defined proteins (e.g. the Src family kinases, c-Abl, and Jak kinases) and other kinases which regulates cell growth and differentiation. For example, Src family kinases are curial for activating and inhibitory pathways in the innate immune response.
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A3750 Regorafenib hydrochlorideTarget: Raf|VEGFR|PDGFR|c-Kit|c-RETSummary: Tyrosine kinase inhibitor
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A3843 SU 5402Target: VEGFR|PDGFR|FGFRSummary: VEGFR2/FGFR/PDGFR/EGFR inhibitor
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B2171 Imatinib (STI571)Target: PDGFR|c-Kit|Bcr-AblSummary: Protein-tyrosine kinase inhibitor
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A8370 Axitinib (AG 013736)1 CitationTarget: VEGFR|PDGFR|c-KitSummary: VEGFR1/ c-Kit inhibitor
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A8476 MK-2461Target: FLT3|PDGFR|MET|RonSummary: C-Met (WT/mutants) inhibitor
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A8550 Telatinib (BAY 57-9352)Target: VEGFR|PDGFR|c-KitSummary: VEGFR-2/-3,PDGFR-β and c-Kit inhibitor
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A3022 Pazopanib (GW-786034)Target: CSF-1R|VEGFR|PDGFR|c-Kit|FGFRSummary: VEGFR/PDGFR/FGFR inhibitor
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B2173 CP-673451Target: PDGFRSummary: PDGFRα/β inhibitor,potent and selective
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A8236 Regorafenib4 CitationTarget: Raf|VEGFR|PDGFR|c-Kit|RETSummary: Inhibitor of VEGFR/PDGFR/FGFR/mutant kit/RET/Raf-1
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A8252 Nintedanib (BIBF 1120)3 CitationTarget: VEGFR|PDGFR|FGFRSummary: VEGFR/PDGFR/FGFR inhibitor