Tyrosine Kinase - Breast Cancer - Chronic Lymphocytic Leukemia - Leukemia - Colon Carcinoma
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.
- B5859 Entrectinib中文名: 恩曲替尼Target: Trk Receptors|ALK|ROS1Summary: ALK激酶抑制剂
- B5854 Pexidartinib (PLX3397)3 Citation中文名: 培西达替尼Target: FLT3|c-Kit|CSF1RSummary: CSF-1R抑制剂
- B4899 BLZ9451 CitationTarget: CSF-1RSummary: CSF-1R激酶抑制剂
- B3553 GS-9973Target: SykSummary: Syk抑制剂
- B2173 CP-673451Target: PDGFRSummary: PDGFRα/β抑制剂
- A8555 Vandetanib (ZD6474)中文名: 凡德他尼Target: VEGFR|EGFRSummary: VEGFR2/EGFR拮抗剂
- A8528 TAK-285Target: EGFR|HER2Summary: HER2/EGFR(HER1)抑制剂
- A8375 AZD8931 (Sapitinib)中文名: 沙普替尼Target: EGFR|ErbBSummary: ErbB抑制剂
- A8370 Axitinib (AG 013736)1 Citation中文名: 阿西替尼Target: VEGFR|PDGFR|c-KitSummary: VEGFR1/ c-Kit抑制剂
- A8366 ARRY-380Target: HER2Summary: 酪氨酸激酶HER2和P95-HER2抑制剂。