Tyrosine Kinase - CSF-1R - ALK - VEGFR - STAT
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.
- C3342 MAZ51Target: VEGFRSummary: VEGFR3拮抗剂
- B5953 Dovitinib (TKI258) LactateTarget: CSF-1R|FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 酪氨酸激酶抑制剂(TKI)
- B5864 Fruquintinib(HMPL-013)中文名: 呋喹替尼Target: VEGFRSummary: VEGFR1\2和3抑制剂
- 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
- B5832 Altiratinib1 CitationTarget: FLT3|VEGFR|Trk Receptors|c-MET|Tie-2Summary: c-MET/TIE-2/VEGFR抑制剂
- B4904 ACTB-1003Target: VEGFR|FGFR|Tie-2|RSK|p70 S6KSummary: FGFR1抑制剂
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- B4882 PF-06463922中文名: 劳拉替尼Target: ALK|ROS1Summary: ALK/ROS1的强效选择性抑制剂
- B1439 Golvatinib (E7050)Target: VEGFRSummary: C-Met/VEGFR-2抑制剂