Tyrosine Kinase
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.
- A8706 BLU9931Target: FGFRSummary: FGFR4 inhibitor,potent and irreversible
- B5843 CTX0294885Target: KinasesSummary: Pan-kinase inhibitor
- B6054 EAI045Summary: Inhibitor of L858R/T790M EGFR mutants
- C5826 AG957Summary: a tyrphostin that targets transforming Bcr-Abl fusion proteins
- B5308 ER 27319 maleateSummary: Selective inhibitor of Syk kinase
- B5456 HKI 357Summary: irreversible inhibitor of ErbB2 (HER2) and EGFR
- B5484 7,8-DihydroxyflavoneSummary: Tyrosine kinase receptor B (TrkB) agonist
- B5516 5'-FluoroindirubinoximeSummary: FMS-like receptor tyrosine kinase-3 (FLT3) inhibitor
- B5611 DMH41 CitationSummary: VEGFR-2 inhibitor
- B5621 Y 11Summary: focal adhesion kinase (FAK) inhibitor