Tyrosine Kinase - CSF-1R - ALK - VEGFR
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.
- A5467 Ponatinib (AP24534)1 Citation中文名: 帕纳替尼Target: VEGFR|PDGFR|Bcr-Abl|FGFR|SrcSummary: pan-BCR-ABL抑制剂,多激酶抑制剂
- A1778 Vatalanib (PTK787) 2HCl中文名: 瓦他拉尼二盐酸盐Target: VEGFRSummary: 酪氨酸激酶受体抑制剂
- A5057 MGCD-265Target: VEGFR|c-METSummary: Met/Flt/Flk/Ron/Tie-2抑制剂
- A2174 Lenvatinib (E7080)中文名: 乐伐替尼,仑伐替尼Target: VEGFR|PDGFR|RETSummary: VEGFR抑制剂
- A2597 Brivanib (BMS-540215)中文名: 布立尼布Target: VEGFR|FGFR|Flk1Summary: VEGFR-2的ATP竞争性抑制剂
- A2251 Tivozanib (AV-951)中文名: 替沃扎尼Target: VEGFRSummary: 有效的VEGFR选择性抑制剂
- A2412 CP-724714Target: VEGFR|PDGFR|Bcr-Abl|Src|EGFR|c-MET|Insulin Receptors|IRG-1RSummary: 有效的HER2选择性抑制剂
- A1882 Cediranib (AZD217)中文名: 西地尼布Target: VEGFRSummary: VEGFR受体高度有效的抑制剂
- A2168 Dovitinib (TKI-258, CHIR-258)2 Citation中文名: 多韦替尼Target: FLT3|VEGFR|PDGFR|c-Kit|FGFRSummary: 多靶点RTK抑制剂
- A2949 Linifanib (ABT-869)Target: VEGFR|PDGFRSummary: VEGFR/PDGFR抑制剂