Tyrosine Kinase - AXL - Tie-2 - p70 S6K - ErbB
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.
- B5940 TP-0903中文名: 度博替尼Target: AXLSummary: AXL受体酪氨酸激酶抑制剂,抗癌药
- B5832 Altiratinib1 CitationTarget: FLT3|VEGFR|Trk Receptors|c-MET|Tie-2Summary: c-MET/TIE-2/VEGFR抑制剂
- B4904 ACTB-1003Target: VEGFR|FGFR|Tie-2|RSK|p70 S6KSummary: FGFR1抑制剂
- B1543 Mubritinib (TAK 165)中文名: 木利替尼Target: ErbBSummary: HER2/ErbB2有效抑制剂
- B1404 DCC-2036 (Rebastinib)Target: FLT3|Bcr-Abl|Tie-2|KDRSummary: Bcr-Abl抑制剂
- A8375 AZD8931 (Sapitinib)中文名: 沙普替尼Target: EGFR|ErbBSummary: ErbB抑制剂
- A8319 Dacomitinib (PF299804, PF299)中文名: 达克替尼Target: ErbBSummary: HER抑制剂
- A5979 Tie2 kinase inhibitor中文名: Tie2激酶抑制剂Target: Tie-2Summary: Tie-2(Tie2 )抑制剂
- A8218 Lapatinib2 Citation中文名: 拉帕替尼Target: ErbBSummary: EGFR/HER2抑制剂
- A4092 CUDC-1011 CitationTarget: Histone Deacetylases (HDACs)|EGFR|ErbBSummary: 多靶点HDAC抑制剂