Tyrosine Kinase - Lyn kinase - c-MET - PKA - IRAK
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.
- B5832 Altiratinib1 CitationTarget: FLT3|VEGFR|Trk Receptors|c-MET|Tie-2Summary: c-MET/TIE-2/VEGFR抑制剂
- B5648 MLR 1023Target: Lyn kinaseSummary: Lyn激酶的变构激活剂
- B6342 H-7 dihydrochlorideTarget: PKC|PKG|PKA|Myosin light chain kinases (MLCKs)Summary: 蛋白激酶抑制剂
- A8448 INCB28060中文名: 苯扎米特Target: c-METSummary: C-Met抑制剂
- A5057 MGCD-265Target: VEGFR|c-METSummary: Met/Flt/Flk/Ron/Tie-2抑制剂
- 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
- A5096 PF-04217903Target: c-METSummary: C-Met的选择性和ATP竞争性抑制剂
- A2307 PHA-6657521 CitationTarget: c-METSummary: c-Met的ATP竞争性、有效的、选择性抑制剂
- A3712 PF-04217903 methanesulfonateTarget: c-METSummary: c-Met抑制剂
- A3505 IRAK-1-4 Inhibitor I3 CitationTarget: IRAKSummary: IRAK-1/4抑制剂