Li Leiming, Okura Masaya, Imamoto Akira
The Ben May Institute for Cancer Research and Center for Molecular Oncology, Committee on Cell Physiology, The University of Chicago, Chicago, Illinois 60637, USA.
Mol Cell Biol. 2002 Feb;22(4):1203-17. doi: 10.1128/MCB.22.4.1203-1217.2002.
Members of the Src family of tyrosine kinases function to phosphorylate focal adhesion (FA) proteins. To explore the overlapping functions of Src kinases, we have targeted Csk, a negative regulator of the Src family, to FA structures. Expression of FA-targeted Csk (FA-Csk) effectively reduced the active form (nonphosphorylated at the C-terminal regulatory tyrosine) of Src members in the cell. We found that fibroblasts expressing FA-Csk lost integrin-mediated adhesion. Activated Src (SrcY529F) as well as activation of putative Src signaling mediators (Fak, Cas, Crk/CrkL, C3G, and Rap1) blocked the effect of FA-Csk in a manner dependent on Rap1. SrcY529F also inhibited activated Ras-induced cell detachment but failed to rescue detachment caused by an activated mutant of Raf1 (Raf-BXB) that Rap1 cannot inhibit. Although normal spreading onto fibronectin was restored by the beta(1) integrin affinity-activating antibody TS2/16 in cells expressing FA-Csk or Raf-BXB, FAs were lost in these cells. On the other hand, Rap1 activation could restore FAs in cells expressing FA-Csk. Activation of the executioner caspase, caspase 3, is essential for many forms of apoptosis. While a caspase 3 inhibitor (Z-DEVD-FMK) inhibited cell detachment triggered by activation of caspase 8, this inhibitor had no effect on cell detachment caused by FA-Csk. Likewise, overexpression of an activated Akt made cells resistant to the effect of caspase 8 activation, but not to the effect of FA-Csk. It is therefore likely that the primary cause of cell rounding and detachment induced by FA-Csk involves dysfunction of FAs rather than caspase-mediated apoptosis that may result from possible loss of survival signals mediated by Src family kinases. We suggest that endogenous Src family kinases are essential for FAs through activation of Rap1 in fibroblasts.
酪氨酸激酶Src家族成员的作用是使粘着斑(FA)蛋白磷酸化。为了探究Src激酶的重叠功能,我们将Src家族的负调控因子Csk靶向到FA结构上。靶向FA的Csk(FA-Csk)的表达有效降低了细胞中Src家族成员的活性形式(C末端调节性酪氨酸未磷酸化)。我们发现,表达FA-Csk的成纤维细胞失去了整合素介导的粘附。活化的Src(SrcY529F)以及假定的Src信号介质(Fak、Cas、Crk/CrkL、C3G和Rap1)的激活以依赖Rap1的方式阻断了FA-Csk的作用。SrcY529F也抑制活化的Ras诱导的细胞脱离,但未能挽救由Rap1无法抑制的Raf1活化突变体(Raf-BXB)引起的脱离。尽管在表达FA-Csk或Raf-BXB的细胞中,β(1)整合素亲和力激活抗体TS2/16可恢复正常铺展在纤连蛋白上,但这些细胞中的粘着斑丢失了。另一方面,Rap1激活可恢复表达FA-Csk的细胞中的粘着斑。刽子手半胱天冬酶caspase 3的激活对多种形式的细胞凋亡至关重要。虽然caspase 3抑制剂(Z-DEVD-FMK)抑制了由caspase 8激活引发的细胞脱离,但该抑制剂对FA-Csk引起的细胞脱离没有影响。同样,活化的Akt过表达使细胞对caspase 8激活的作用产生抗性,但对FA-Csk的作用没有抗性。因此,FA-Csk诱导细胞变圆和脱离的主要原因可能是粘着斑功能障碍,而不是可能由Src家族激酶介导的存活信号丧失导致的caspase介导的细胞凋亡。我们认为,内源性Src家族激酶通过在成纤维细胞中激活Rap1对粘着斑至关重要。