Tyrosine Kinase - KDR - Insulin and Insulin-like Receptors
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.
- B1404 DCC-2036 (Rebastinib)Target: FLT3|Bcr-Abl|Tie-2|KDRSummary: Bcr-Abl抑制剂
- A8440 GSK1838705ATarget: Insulin and Insulin-like Receptors|ALKSummary: ATP竞争性IGF-IR/IR/ALK抑制剂
- A1302 GSK1904529ATarget: Insulin and Insulin-like ReceptorsSummary: IGF-1R/IR 选择性抑制剂
- A1185 BMS-754807Target: Insulin and Insulin-like ReceptorsSummary: 有效的、选择性的IGF-1R和InsR抑制剂