Tyrosine Kinase - ErbB-2 - c-Kit - Src
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)
- B5854 Pexidartinib (PLX3397)3 Citation中文名: 培西达替尼Target: FLT3|c-Kit|CSF1RSummary: CSF-1R抑制剂
- B5839 SU6656Target: Src|Lyn|YES|FynSummary: Src 酪氨酸激酶抑制剂
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- B5673 KB SRC 4Target: SrcSummary: c-Src抑制剂
- B2171 Imatinib (STI571)中文名: 伊马替尼Target: PDGFR|c-Kit|Bcr-AblSummary: 蛋白酪氨酸激酶抑制剂
- B1299 1-NM-PP1Target: Cyclin-Dependent Kinases|Bcr-Abl|Src|Ca2 /calmodulin-dependent protein kinases (CaMKs)|c-FynSummary: Pp60c-src抑制剂
- A8812 PD173955Target: Bcr-Abl|SrcSummary: Src/Abl激酶双重抑制剂
- A8550 Telatinib (BAY 57-9352)中文名: 替拉替尼Target: VEGFR|PDGFR|c-KitSummary: VEGFR-2/-3、PDGFR-β和c-Kit抑制剂
- A8370 Axitinib (AG 013736)1 Citation中文名: 阿西替尼Target: VEGFR|PDGFR|c-KitSummary: VEGFR1/ c-Kit抑制剂