Tyrosine Kinase - Acute Myelogenous Leukemia - Glioblastoma - Pancreatic 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
- B5854 Pexidartinib (PLX3397)3 Citation中文名: 培西达替尼Target: FLT3|c-Kit|CSF1RSummary: CSF-1R抑制剂
- B8016 UNC20251 CitationTarget: MER|FLT3Summary: 口服生物可利用的双重MER/FLT3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
- A8476 MK-2461Target: FLT3|PDGFR|MET|RonSummary: C-Met(野生型/突变型)抑制剂
- A8345 PF-562271 HClTarget: FAK|Pyk2Summary: FAK/Pyk2抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met抑制剂
- A8320 PF-00562271Target: FAK|Pyk2Summary: 有效的ATP竞争性FAK/Pyk2抑制剂