Tyrosine Kinase - Cell Experiments - Pancreatic Cancer - Cholangiocarcinoma - Colorectal Cancer
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.
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- A8476 MK-2461Target: FLT3|PDGFR|MET|RonSummary: C-Met(野生型/突变型)抑制剂
- A8345 PF-562271 HClTarget: FAK|Pyk2Summary: FAK/Pyk2抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met抑制剂
- A8320 PF-00562271Target: FAK|Pyk2Summary: 有效的ATP竞争性FAK/Pyk2抑制剂
- A1882 Cediranib (AZD217)中文名: 西地尼布Target: VEGFRSummary: VEGFR受体高度有效的抑制剂
- A2168 Dovitinib (TKI-258, CHIR-258)2 Citation中文名: 多韦替尼Target: FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 多靶点RTK抑制剂
- A2678 SU112742 CitationTarget: METSummary: C-Met抑制剂
- A8252 Nintedanib (BIBF 1120)3 Citation中文名: 尼达尼布Target: VEGFR|PDGFR|FGFRSummary: VEGFR/PDGFR/FGFR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