Tyrosine Kinase - Renal Cell Carcinoma - Glioma - Thyroid Cancer - Colorectal Cancer
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.
- B5859 Entrectinib中文名: 恩曲替尼Target: Trk Receptors|ALK|ROS1Summary: ALK激酶抑制剂
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- A8557 TAE226 (NVP-TAE226)1 CitationTarget: FAKSummary: 强效的ATP竞争性FAK抑制剂
- A8370 Axitinib (AG 013736)1 Citation中文名: 阿西替尼Target: VEGFR|PDGFR|c-KitSummary: VEGFR1/ c-Kit抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met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
- A2174 Lenvatinib (E7080)中文名: 乐伐替尼,仑伐替尼Target: VEGFR|PDGFR|RETSummary: VEGFR抑制剂
- A2251 Tivozanib (AV-951)中文名: 替沃扎尼Target: VEGFRSummary: 有效的VEGFR选择性抑制剂
- A1882 Cediranib (AZD217)中文名: 西地尼布Target: VEGFRSummary: VEGFR受体高度有效的抑制剂