Tyrosine Kinase - MER - insulin - S1P receptors - MET
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.
- B8016 UNC20251 CitationTarget: MER|FLT3Summary: 口服生物可利用的双重MER/FLT3抑制剂
- B1438 BMS-794833Target: MET|Flk-1Summary: Met/VEGFR2抑制剂
- A8548 Fingolimod (FTY720)中文名: 盐酸芬戈莫德Target: S1P receptorsSummary: S1P受体激动剂
- A8476 MK-2461Target: FLT3|PDGFR|MET|RonSummary: C-Met(野生型/突变型)抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met抑制剂
- A2024 PD168393Target: PDGFR|FGFR|EGFR|PKC|insulinSummary: EGFR抑制剂
- A5703 BMS-777607Target: METSummary: 强效的c-Met选择性抑制剂
- A1196 SGX-5231 CitationTarget: METSummary: 高度选择性的、ATP竞争性的Met抑制剂
- A2678 SU112742 CitationTarget: METSummary: C-Met抑制剂
- A3573 LY2801653Target: METSummary: MET抑制剂