Tyrosine Kinase - Non-small Cell Lung Cancer - Colon 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.
- B5889 EGF8162 Citation中文名: 那扎替尼Target: EGFRSummary: EGFR突变选择性抑制剂
- A8555 Vandetanib (ZD6474)中文名: 凡德他尼Target: VEGFR|EGFRSummary: VEGFR2/EGFR拮抗剂
- A8393 CH5424802中文名: 阿来替尼Target: ALKSummary: ALK的有效ATP竞争性抑制剂
- A5057 MGCD-265Target: VEGFR|c-METSummary: Met/Flt/Flk/Ron/Tie-2抑制剂
- A8247 Afatinib (BIBW2992)1 Citation中文名: 阿法替尼Target: EGFRSummary: EGFR/ HER2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
- A3632 Motesanib中文名: 莫特塞尼Target: VEGFRSummary: Flk-1/Flt-4/PDGFR-/c-Kit抑制剂
- A3433 Gefitinib hydrochloride中文名: 盐酸吉非替尼Target: EGFRSummary: EGFR有效的抑制剂
- 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。