Tyrosine Kinase - c-Fms tyrosine kinase - ALK - ErbB-2
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
- B4882 PF-06463922中文名: 劳拉替尼Target: ALK|ROS1Summary: ALK/ROS1的强效选择性抑制剂
- A8620 AZD-34633 CitationTarget: ALK|Insulin-like growth factors (IGFs)Summary: ALK/IGF1R抑制剂
- A8393 CH5424802中文名: 阿来替尼Target: ALKSummary: ALK的有效ATP竞争性抑制剂
- A8440 GSK1838705ATarget: Insulin and Insulin-like Receptors|ALKSummary: ATP竞争性IGF-IR/IR/ALK抑制剂
- A8328 LDK378中文名: 色瑞替尼Target: ALKSummary: 强效的ALK抑制剂
- A3967 Lapatinib Ditosylate中文名: 二苯磺酸拉帕替尼Target: EGFR|ErbB-2Summary: EGFR / HER2抑制剂
- A3527 Ki20227Target: c-Fms tyrosine kinaseSummary: C-Fms酪氨酸激酶抑制剂