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.
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- C5553 HNMPASummary: 细胞非渗透性酪氨酸激酶抑制剂
- C4770 AG-213Summary: 表皮生长因子(EGF)受体激酶抑制剂
- C4766 RG-14620Summary: 表皮生长因子(EGF)受体激酶抑制剂
- C4760 AG-82Summary: EGFR激酶抑制剂
- C4603 VEGFR Tyrosine Kinase Inhibitor II1 CitationSummary: VEGFR抑制剂
- C4539 AG-370Summary: PDGFR抑制剂
- C4541 LDN-211904Summary: 促红细胞生成素产生肝细胞癌(Eph)受体的抑制剂
- C4439 PKR InhibitorSummary: 双链RNA激活蛋白激酶(PKR)抑制剂