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.
- B6054 EAI045Summary: Inhibitor of L858R/T790M EGFR mutants
- B5843 CTX0294885Target: KinasesSummary: Pan-kinase inhibitor
- A8706 BLU9931Target: FGFRSummary: FGFR4 inhibitor,potent and irreversible
- C5826 AG957Summary: a tyrphostin that targets transforming Bcr-Abl fusion proteins
- C5465 AG-1295Summary: potent and selective inhibitor of PDGF receptor kinase
- C5417 AG-1557Summary: inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase
- C4953 HA-100 (hydrochloride)Summary: inhibitor of protein kinases (PKs)
- C4844 AG-183Summary: inhibitor of epidermal growth factor (EGF) receptor kinase
- B7853 Tandutinib (MLN518) HClSummary: FLT3 inhibitor,potent and selective
- C5553 HNMPASummary: cell impermeable tyrosine kinase inhibitor