Tyrosine Kinase - FGFR
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.
- A8706 BLU9931Target: FGFRSummary: 有效的FGFR4不可逆抑制剂
- B5953 Dovitinib (TKI258) LactateTarget: CSF-1R|FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 酪氨酸激酶抑制剂(TKI)
- B4904 ACTB-1003Target: VEGFR|FGFR|Tie-2|RSK|p70 S6KSummary: FGFR1抑制剂
- A8696 FIIN-2Target: FGFRSummary: FGFR抑制剂
- A8350 AZD4547Target: FGFRSummary: FGFR抑制剂
- A2024 PD168393Target: PDGFR|FGFR|EGFR|PKC|insulinSummary: EGFR抑制剂
- A5467 Ponatinib (AP24534)1 Citation中文名: 帕纳替尼Target: VEGFR|PDGFR|Bcr-Abl|FGFR|SrcSummary: pan-BCR-ABL抑制剂,多激酶抑制剂
- A2597 Brivanib (BMS-540215)中文名: 布立尼布Target: VEGFR|FGFR|Flk1Summary: VEGFR-2的ATP竞争性抑制剂
- A2168 Dovitinib (TKI-258, CHIR-258)2 Citation中文名: 多韦替尼Target: FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 多靶点RTK抑制剂
- A8253 PD 173074Target: VEGFR|FGFRSummary: FGFR抑制剂