Tyrosine Kinase - Irreversible
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
- B5889 EGF8162 Citation中文名: 那扎替尼Target: EGFRSummary: EGFR突变选择性抑制剂
- A8696 FIIN-2Target: FGFRSummary: FGFR抑制剂
- B1104 AZD-92911 Citation中文名: 奥希替尼Target: EGFRSummary: 突变型EGFR抑制剂。
- A8322 Neratinib (HKI-272)1 Citation中文名: 来那替尼Target: EGFRSummary: HER2/EGFR抑制剂
- A8319 Dacomitinib (PF299804, PF299)中文名: 达克替尼Target: ErbBSummary: HER抑制剂
- A2024 PD168393Target: PDGFR|FGFR|EGFR|PKC|insulinSummary: EGFR抑制剂
- A8247 Afatinib (BIBW2992)1 Citation中文名: 阿法替尼Target: EGFRSummary: EGFR/ HER2抑制剂