Tyrosine Kinase - Glioblastoma
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.
- B5854 Pexidartinib (PLX3397)3 Citation中文名: 培西达替尼Target: FLT3|c-Kit|CSF1RSummary: CSF-1R抑制剂
- B1438 BMS-794833Target: MET|Flk-1Summary: Met/VEGFR2抑制剂
- B2173 CP-673451Target: PDGFRSummary: PDGFRα/β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
- A1196 SGX-5231 CitationTarget: METSummary: 高度选择性的、ATP竞争性的Met抑制剂
- A8236 Regorafenib4 Citation中文名: 瑞戈非尼Target: Raf|VEGFR|PDGFR|c-Kit|RETSummary: VEGFR/PDGFR/FGFR/mutant Kit/RET/Raf-1抑制剂
- A8219 Gefitinib (ZD1839)3 Citation中文名: 吉非替尼Target: EGFRSummary: EGFR抑制剂
- A3433 Gefitinib hydrochloride中文名: 盐酸吉非替尼Target: EGFRSummary: EGFR有效的抑制剂
- 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。