Tyrosine Kinase
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.
- C3485 SR 1555 (hydrochloride)Summary: RORγ的反向激动剂
- C3415 Tivozanib (hydrate)Summary: 口服可用的VEGFR抑制剂
- C3342 MAZ51Target: VEGFRSummary: VEGFR3拮抗剂
- C3327 EGFR InhibitorSummary: EGFR抑制剂
- C3285 EGFR/ErbB2 InhibitorSummary: EGFR和c-ErbB2抑制剂
- C3152 ISCK03Summary: SCF介导的c-kit激活的抑制剂
- B7815 NSC228155Summary: EGFR激活剂
- B7813 Olmutinib (HM61713, BI 1482694)中文名: 奥莫替尼Summary: EGFR突变特异性抑制剂
- B7808 NT1571 CitationSummary: IRS-1/2抑制剂,抑制IGF-1R和STAT3信号通路
- B7800 BAW2881 (NVP-BAW2881)Summary: VEGFR抑制剂