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.
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- B4893 LDC1267Target: TAM kinaseSummary: TAM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
- B8016 UNC20251 CitationTarget: MER|FLT3Summary: 口服生物可利用的双重MER/FLT3抑制剂
- B3553 GS-9973Target: SykSummary: Syk抑制剂
- B5712 ANA 121 CitationTarget: Trk ReceptorsSummary: TrkB受体拮抗剂
- B5673 KB SRC 4Target: SrcSummary: c-Src抑制剂
- B5648 MLR 1023Target: Lyn kinaseSummary: Lyn激酶的变构激活剂
- B7354 SU 16fTarget: PDGFRSummary: PDGFRβ抑制剂
- B6342 H-7 dihydrochlorideTarget: PKC|PKG|PKA|Myosin light chain kinases (MLCKs)Summary: 蛋白激酶抑制剂