Tyrosine Kinase - Thyroid Cancer - Myeloma
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.
- A2174 Lenvatinib (E7080)中文名: 乐伐替尼,仑伐替尼Target: VEGFR|PDGFR|RETSummary: VEGFR抑制剂
- A3632 Motesanib中文名: 莫特塞尼Target: VEGFRSummary: Flk-1/Flt-4/PDGFR-/c-Kit抑制剂
- A3209 AXL1717中文名: 鬼臼毒素Target: Insulin-like growth factor receptors(IGFRs)Summary: IGF-1R抑制剂,口服有效。
- A3194 AST 4871 CitationTarget: RETSummary: RET激酶抑制剂
- A3009 Sorafenib2 Citation中文名: 索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂