Tyrosine Kinase - Lung Cancer
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.
- B3686 DMH-1Target: BMP and Other Activin ReceptorsSummary: BMP ALK2受体抑制剂
- A8350 AZD4547Target: FGFRSummary: FGFR抑制剂
- A5703 BMS-777607Target: METSummary: 强效的c-Met选择性抑制剂
- A1882 Cediranib (AZD217)中文名: 西地尼布Target: VEGFRSummary: VEGFR受体高度有效的抑制剂
- A8215 PP 1Target: Src|EGFR|JAK|ZAP-70Summary: Src家族酪氨酸激酶抑制剂
- A3632 Motesanib中文名: 莫特塞尼Target: VEGFRSummary: Flk-1/Flt-4/PDGFR-/c-Kit抑制剂
- A3165 ALW-II-41-271 CitationTarget: Eph ReceptorsSummary: Eph受体抑制剂
- A3020 (R)-Crizotinib2 Citation中文名: 克唑替尼Target: c-METSummary: ATP竞争性的C-MET/ALK抑制剂。