Tyrosine Kinase - Insulin and Insulin-like Receptors - Syk - Bcr-Abl
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.
- B3553 GS-9973Target: SykSummary: Syk抑制剂
- B2171 Imatinib (STI571)中文名: 伊马替尼Target: PDGFR|c-Kit|Bcr-AblSummary: 蛋白酪氨酸激酶抑制剂
- B1299 1-NM-PP1Target: Cyclin-Dependent Kinases|Bcr-Abl|Src|Ca2 /calmodulin-dependent protein kinases (CaMKs)|c-FynSummary: Pp60c-src抑制剂
- B2284 Fostamatinib (R788)中文名: 福坦替尼Target: SykSummary: 脾酪氨酸激酶(Syk)抑制剂
- B1404 DCC-2036 (Rebastinib)Target: FLT3|Bcr-Abl|Tie-2|KDRSummary: Bcr-Abl抑制剂
- B1402 GZD824Target: Bcr-AblSummary: Bcr-Abl抑制剂
- A8812 PD173955Target: Bcr-Abl|SrcSummary: Src/Abl激酶双重抑制剂
- A8604 GNF 5Target: Bcr-AblSummary: Bcr-Abl抑制剂
- A8546 R4061 CitationTarget: SykSummary: SYK抑制剂
- A8440 GSK1838705ATarget: Insulin and Insulin-like Receptors|ALKSummary: ATP竞争性IGF-IR/IR/ALK抑制剂