Tyrosine Kinase - Clear Cell Renal Cell Carcinoma - Rheumatoid Arthritis - Acute Myeloid Leukemia
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.
- B2284 Fostamatinib (R788)中文名: 福坦替尼Target: SykSummary: 脾酪氨酸激酶(Syk)抑制剂
- A8350 AZD4547Target: FGFRSummary: FGFR抑制剂
- A8332 R788 disodium中文名: 福他替尼二钠盐Target: SykSummary: Syk的ATP竞争性抑制剂
- A8307 Crenolanib (CP-868596)1 Citation中文名: 克莱拉尼Target: FLT3|PDGFRSummary: PDGFR-β有效的选择性抑制剂
- A5793 Quizartinib (AC220)中文名: 奎扎替尼Target: FLT3Summary: FLT3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
- A8232 Nilotinib(AMN-107)1 Citation中文名: 尼洛替尼Target: Bcr-AblSummary: 选择性Bcr-Abl 激酶抑制剂
- A3573 LY2801653Target: METSummary: MET抑制剂