Tyrosine Kinase - IRG-1R - AXL - Fyn kinase - Insulin-like growth factor receptors(IGFRs)
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.
- B5940 TP-0903中文名: 度博替尼Target: AXLSummary: AXL受体酪氨酸激酶抑制剂,抗癌药
- A2412 CP-724714Target: VEGFR|PDGFR|Bcr-Abl|Src|EGFR|c-MET|Insulin Receptors|IRG-1RSummary: 有效的HER2选择性抑制剂
- A3870 TG 100801Target: VEGFR|FGFR|Src|Fyn kinaseSummary: 多激酶抑制剂
- A3209 AXL1717中文名: 鬼臼毒素Target: Insulin-like growth factor receptors(IGFRs)Summary: IGF-1R抑制剂,口服有效。