Tyrosine Kinase - Cervical Cancer - Lung Cancer - Acute Myeloid Leukemia - Colorectal 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.
- B5859 Entrectinib中文名: 恩曲替尼Target: Trk Receptors|ALK|ROS1Summary: ALK激酶抑制剂
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- B3686 DMH-1Target: BMP and Other Activin ReceptorsSummary: BMP ALK2受体抑制剂
- A8370 Axitinib (AG 013736)1 Citation中文名: 阿西替尼Target: VEGFR|PDGFR|c-KitSummary: VEGFR1/ c-Kit抑制剂
- A8350 AZD4547Target: FGFRSummary: FGFR抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met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