Tyrosine Kinase - Clear Cell Renal Cell Carcinoma - Renal Cell Carcinoma - Hepatocellular Carcinoma - Pulmonary Arterial Hypertension
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.
- A8370 Axitinib (AG 013736)1 Citation中文名: 阿西替尼Target: VEGFR|PDGFR|c-KitSummary: VEGFR1/ c-Kit抑制剂
- A8345 PF-562271 HClTarget: FAK|Pyk2Summary: FAK/Pyk2抑制剂
- A8325 Tivantinib (ARQ 197)2 CitationTarget: METSummary: C-Met抑制剂
- A8320 PF-00562271Target: FAK|Pyk2Summary: 有效的ATP竞争性FAK/Pyk2抑制剂
- A5602 SB525334Summary: TGF-beta1受体抑制剂
- A2251 Tivozanib (AV-951)中文名: 替沃扎尼Target: VEGFRSummary: 有效的VEGFR选择性抑制剂
- 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
- A8255 Sunitinib malate2 Citation中文名: 苹果酸舒尼替尼Target: VEGFRSummary: VEGFR/PDGFRβ/ KIT/ FLT3/RET/CSF-1R抑制剂