Tyrosine Kinase - Raf - CSF-1R
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.
- B5953 Dovitinib (TKI258) LactateTarget: CSF-1R|FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 酪氨酸激酶抑制剂(TKI)
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- A8313 RAF265Target: Raf|VEGFRSummary: 多细胞激酶抑制剂
- A1655 GW25801 CitationTarget: CSF-1RSummary: CFMS激酶/CSF-1R抑制剂
- A8245 Sorafenib Tosylate1 Citation中文名: 甲苯磺酸索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂
- A8236 Regorafenib4 Citation中文名: 瑞戈非尼Target: Raf|VEGFR|PDGFR|c-Kit|RETSummary: VEGFR/PDGFR/FGFR/mutant Kit/RET/Raf-1抑制剂
- A3750 Regorafenib hydrochloride中文名: 瑞戈非尼盐酸盐Target: Raf|VEGFR|PDGFR|c-Kit|c-RETSummary: 酪氨酸激酶抑制剂
- A3022 Pazopanib (GW-786034)中文名: 帕唑帕尼Target: CSF-1R|VEGFR|PDGFR|c-Kit|FGFRSummary: (GW-786034)VEGFR/PDGFR/FGFR 的抑制剂。
- A3009 Sorafenib2 Citation中文名: 索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂