Tyrosine Kinase - ZAP-70 - Src - FAK - 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.
- B4800 Defactinib中文名: 地法替尼Target: FAKSummary: FAK磷酸化抑制剂
- A8557 TAE226 (NVP-TAE226)1 CitationTarget: FAKSummary: 强效的ATP竞争性FAK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。
- A2133 Saracatinib (AZD0530)3 Citation中文名: 塞卡替尼Target: SrcSummary: Src/Abl抑制剂
- A2412 CP-724714Target: VEGFR|PDGFR|Bcr-Abl|Src|EGFR|c-MET|Insulin Receptors|IRG-1RSummary: 有效的HER2选择性抑制剂
- A2149 Bosutinib (SKI-606)1 Citation中文名: 伯舒替尼Target: Bcr-Abl|SrcSummary: Abl/Src有效的抑制剂
- A8215 PP 1Target: Src|EGFR|JAK|ZAP-70Summary: Src家族酪氨酸激酶抑制剂
- A3535 KX2-391 dihydrochlorideTarget: SrcSummary: Src激酶抑制剂