Tyrosine Kinase - ROS1 - Pyk2
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
- A8345 PF-562271 HClTarget: FAK|Pyk2Summary: FAK/Pyk2抑制剂
- A8320 PF-00562271Target: FAK|Pyk2Summary: 有效的ATP竞争性FAK/Pyk2抑制剂
- A8310 PF-5622711 CitationTarget: FAK|Pyk2Summary: ATP竞争性的FAK抑制剂。