Tyrosine Kinase - JAK - PDGFR - RET
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)
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- B7354 SU 16fTarget: PDGFRSummary: PDGFRβ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
- B2173 CP-673451Target: PDGFRSummary: PDGFRα/β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
- A8476 MK-2461Target: FLT3|PDGFR|MET|RonSummary: C-Met(野生型/突变型)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
- A8307 Crenolanib (CP-868596)1 Citation中文名: 克莱拉尼Target: FLT3|PDGFRSummary: PDGFR-β有效的选择性抑制剂
- A2477 Tyrphostin AG 12961 CitationTarget: PDGFRSummary: PDGFR抑制剂