Tyrosine Kinase - Insulin and Insulin-like Receptors - Syk - EGFR
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.
- B5889 EGF8162 Citation中文名: 那扎替尼Target: EGFRSummary: EGFR突变选择性抑制剂
- B3553 GS-9973Target: SykSummary: Syk抑制剂
- B1104 AZD-92911 Citation中文名: 奥希替尼Target: EGFRSummary: 突变型EGFR抑制剂。
- B2284 Fostamatinib (R788)中文名: 福坦替尼Target: SykSummary: 脾酪氨酸激酶(Syk)抑制剂
- A8555 Vandetanib (ZD6474)中文名: 凡德他尼Target: VEGFR|EGFRSummary: VEGFR2/EGFR拮抗剂
- A8546 R4061 CitationTarget: SykSummary: SYK抑制剂
- A8528 TAK-285Target: EGFR|HER2Summary: HER2/EGFR(HER1)抑制剂
- A8440 GSK1838705ATarget: Insulin and Insulin-like Receptors|ALKSummary: ATP竞争性IGF-IR/IR/ALK抑制剂
- A8375 AZD8931 (Sapitinib)中文名: 沙普替尼Target: EGFR|ErbBSummary: ErbB抑制剂
- A8357 AG-1478中文名: 酪氨酸磷酸化抑制剂 AG-1478Target: EGFRSummary: EGFR抑制剂