Tyrosine Kinase - Cell Experiments
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.
- C3342 MAZ51Target: VEGFRSummary: VEGFR3拮抗剂
- B6176 LOXO-101中文名: 硫酸盐拉罗替尼Target: tropomyosin receptor kinaseSummary: 原肌球蛋白受体激酶(TRK)抑制剂
- B5953 Dovitinib (TKI258) LactateTarget: CSF-1R|FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 酪氨酸激酶抑制剂(TKI)
- 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
- B5864 Fruquintinib(HMPL-013)中文名: 呋喹替尼Target: VEGFRSummary: VEGFR1\2和3抑制剂
- B5839 SU6656Target: Src|Lyn|YES|FynSummary: Src 酪氨酸激酶抑制剂
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- B5832 Altiratinib1 CitationTarget: FLT3|VEGFR|Trk Receptors|c-MET|Tie-2Summary: c-MET/TIE-2/VEGFR抑制剂
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- B4893 LDC1267Target: TAM kinaseSummary: TAM激酶抑制剂