Tyrosine Kinase - EGFR - Breast Cancer
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.
- 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
- A8322 Neratinib (HKI-272)1 Citation中文名: 来那替尼Target: EGFRSummary: HER2/EGFR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
- A8219 Gefitinib (ZD1839)3 Citation中文名: 吉非替尼Target: EGFRSummary: EGFR抑制剂
- A3433 Gefitinib hydrochloride中文名: 盐酸吉非替尼Target: EGFRSummary: EGFR有效的抑制剂