Tyrosine Kinase - Mer tyrosine kinase - tropomyosin receptor kinase - ZAP-70 - CSF-1R
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.
- 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)
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- B4357 UNC2881Target: Mer tyrosine kinaseSummary: Mer酪氨酸激酶抑制剂
- A1655 GW25801 CitationTarget: CSF-1RSummary: CFMS激酶/CSF-1R抑制剂
- A8215 PP 1Target: Src|EGFR|JAK|ZAP-70Summary: Src家族酪氨酸激酶抑制剂
- A3022 Pazopanib (GW-786034)中文名: 帕唑帕尼Target: CSF-1R|VEGFR|PDGFR|c-Kit|FGFRSummary: (GW-786034)VEGFR/PDGFR/FGFR 的抑制剂。