Tyrosine Kinase - Flk1 - Aurora Kinases
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.
- A8889 G-749Target: Aurora Kinases|FLT3|c-RETSummary: FLT3抑制剂
- A2597 Brivanib (BMS-540215)中文名: 布立尼布Target: VEGFR|FGFR|Flk1Summary: VEGFR-2的ATP竞争性抑制剂
- A4123 KW 2449Target: Aurora Kinases|FLT3|Bcr-AblSummary: 多重激酶抑制剂
- A4116 Danusertib (PHA-739358)2 Citation中文名: 达鲁舍替Target: Aurora KinasesSummary: Aurora kinase(极光激酶)抑制剂