Tyrosine Kinase - ITK - Raf - PKC - HER2
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.
- B6342 H-7 dihydrochlorideTarget: PKC|PKG|PKA|Myosin light chain kinases (MLCKs)Summary: 蛋白激酶抑制剂
- A8528 TAK-285Target: EGFR|HER2Summary: HER2/EGFR(HER1)抑制剂
- A8366 ARRY-380Target: HER2Summary: 酪氨酸激酶HER2和P95-HER2抑制剂。
- A8313 RAF265Target: Raf|VEGFRSummary: 多细胞激酶抑制剂
- A2024 PD168393Target: PDGFR|FGFR|EGFR|PKC|insulinSummary: EGFR抑制剂
- A8245 Sorafenib Tosylate1 Citation中文名: 甲苯磺酸索拉非尼Target: Raf|VEGFRSummary: Raf激酶和酪氨酸激酶抑制剂
- A8236 Regorafenib4 Citation中文名: 瑞戈非尼Target: Raf|VEGFR|PDGFR|c-Kit|RETSummary: VEGFR/PDGFR/FGFR/mutant Kit/RET/Raf-1抑制剂
- A3750 Regorafenib hydrochloride中文名: 瑞戈非尼盐酸盐Target: Raf|VEGFR|PDGFR|c-Kit|c-RETSummary: 酪氨酸激酶抑制剂
- A3250 BMS-509744Target: ITKSummary: Itk抑制剂
- A3145 Afatinib dimaleate中文名: 马来酸阿法替尼Target: EGFR|HER2Summary: EGFR抑制剂