Tyrosine Kinase - Mer tyrosine kinase - tropomyosin receptor kinase - EGFR - FLT3
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.
- B6176 LOXO-101中文名: 硫酸盐拉罗替尼Target: tropomyosin receptor kinaseSummary: 原肌球蛋白受体激酶(TRK)抑制剂
- B5953 Dovitinib (TKI258) LactateTarget: CSF-1R|FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 酪氨酸激酶抑制剂(TKI)
- B5889 EGF8162 Citation中文名: 那扎替尼Target: EGFRSummary: EGFR突变选择性抑制剂
- B5854 Pexidartinib (PLX3397)3 Citation中文名: 培西达替尼Target: FLT3|c-Kit|CSF1RSummary: CSF-1R抑制剂
- 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
- B8016 UNC20251 CitationTarget: MER|FLT3Summary: 口服生物可利用的双重MER/FLT3抑制剂
- A8889 G-749Target: Aurora Kinases|FLT3|c-RETSummary: FLT3抑制剂
- B4357 UNC2881Target: Mer tyrosine kinaseSummary: Mer酪氨酸激酶抑制剂
- B1104 AZD-92911 Citation中文名: 奥希替尼Target: EGFRSummary: 突变型EGFR抑制剂。