Tyrosine Kinase - Cervical Cancer - Lung Cancer - Acute Myeloid Leukemia - Non-small Cell 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.
- B5889 EGF8162 Citation中文名: 那扎替尼Target: EGFRSummary: EGFR突变选择性抑制剂
- B3686 DMH-1Target: BMP and Other Activin ReceptorsSummary: BMP ALK2受体抑制剂
- A8393 CH5424802中文名: 阿来替尼Target: ALKSummary: ALK的有效ATP竞争性抑制剂
- A8350 AZD4547Target: FGFRSummary: FGFR抑制剂
- A8307 Crenolanib (CP-868596)1 Citation中文名: 克莱拉尼Target: FLT3|PDGFRSummary: PDGFR-β有效的选择性抑制剂
- A5793 Quizartinib (AC220)中文名: 奎扎替尼Target: FLT3Summary: FLT3抑制剂
- A5703 BMS-777607Target: METSummary: 强效的c-Met选择性抑制剂
- A1778 Vatalanib (PTK787) 2HCl中文名: 瓦他拉尼二盐酸盐Target: VEGFRSummary: 酪氨酸激酶受体抑制剂
- A5057 MGCD-265Target: VEGFR|c-METSummary: Met/Flt/Flk/Ron/Tie-2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