Tyrosine Kinase - Selective
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.
- B4633 GNE0877Target: LRRK2Summary: LRRK2抑制剂
- B3688 ML347Target: BMP and Other Activin ReceptorsSummary: 有效的BMP受体选择性抑制剂
- B3686 DMH-1Target: BMP and Other Activin ReceptorsSummary: BMP ALK2受体抑制剂
- B3605 GNE-7915Target: LRRK2Summary: LRRK2抑制剂
- B1438 BMS-794833Target: MET|Flk-1Summary: Met/VEGFR2抑制剂
- B2297 GW4417561 CitationTarget: Trk ReceptorsSummary: TrkA抑制剂
- B1104 AZD-92911 Citation中文名: 奥希替尼Target: EGFRSummary: 突变型EGFR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
- B1262 HG-10-102-011 CitationTarget: LRRK2Summary: LRRK2抑制剂