Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai, P.R. China.
Curr Med Chem. 2010;17(12):1117-24. doi: 10.2174/092986710790827861.
Src family tyrosine kinases (SFKs) play key roles in regulating signal transduction in cellular processes. However, hyper-activated SFKs lead to uncontrolled cell proliferation and cancers. For both Src SH2 and SH3 domains involve in the regulation of tumorigenesis signal pathways, the SH2 and SH3 inhibition strategies are expected to block the protein-protein interactions between SFKs and their corporation proteins to abolish the signal transduction. Many inhibitors of SH2 and SH3 domain have been identified. Herein, some predominant examples of these inhibitors are reviewed.
Src 家族酪氨酸激酶(SFKs)在调节细胞过程中的信号转导中发挥着关键作用。然而,过度激活的 SFKs 导致不受控制的细胞增殖和癌症。由于Src 的 SH2 和 SH3 结构域都参与了肿瘤发生信号通路的调节,因此预计 SH2 和 SH3 抑制策略将阻断 SFKs 与其合作蛋白之间的蛋白质-蛋白质相互作用,从而阻断信号转导。已经鉴定出许多 SH2 和 SH3 结构域的抑制剂。在此,对其中一些主要的抑制剂进行了综述。