Tyrosine Kinase - Liver Cancer - Prostate Cancer - Bladder Cancer - Lung Carcinoma
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.
- B2173 CP-673451Target: PDGFRSummary: PDGFRα/β抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met抑制剂
- A2133 Saracatinib (AZD0530)3 Citation中文名: 塞卡替尼Target: SrcSummary: Src/Abl抑制剂
- A1882 Cediranib (AZD217)中文名: 西地尼布Target: VEGFRSummary: VEGFR受体高度有效的抑制剂
- 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
- A1196 SGX-5231 CitationTarget: METSummary: 高度选择性的、ATP竞争性的Met抑制剂
- A2678 SU112742 CitationTarget: METSummary: C-Met抑制剂
- A1821 Ki8751Target: VEGFRSummary: VEGFR-2有效的、选择性抑制剂
- A8245 Sorafenib Tosylate1 Citation中文名: 甲苯磺酸索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂
- A8219 Gefitinib (ZD1839)3 Citation中文名: 吉非替尼Target: EGFRSummary: EGFR抑制剂