Mak Baldwin C, Kenerson Heidi L, Aicher Lauri D, Barnes Elizabeth A, Yeung Raymond S
Department of Surgery, University of Washington, 1959 NE Pacific St., Box 356410, Seattle, WA 98195, USA.
Am J Pathol. 2005 Jul;167(1):107-16. doi: 10.1016/s0002-9440(10)62958-6.
The pathology associated with tuberous sclerosis complex (TSC) shows diverse phenotypes that suggest abnormal signaling of multiple pathways. Besides the negative regulatory role of the TSC1/TSC2 proteins on mTOR, we have reported an effect on beta-catenin signaling at the level of the degradation complex in vitro. The TSC1/TSC2 complex associates with GSK3 and Axin and promotes beta-catenin degradation to inhibit Wnt-stimulated TCF/LEF-dependent transcription. Here, we show that beta-catenin and its effectors, cyclin D1 and connexin 43, were up-regulated in TSC-related angiomyolipomas and lymphangioleiomyomatosis. This was supported by the failure of three disease-causing TSC2 missense mutants to inhibit Wnt signaling. Further, the interaction between TSC1/TSC2 and components of the beta-catenin degradation complex was dependent on Wnt stimulation such that binding of tuberin to GSK3 and Axin was reduced in the presence of Wnt whereas the tuberin-Dishevelled interaction was increased. GSK3 activity played a role in regulating the assembly/stability of the degradation complex. Inhibition of GSK3 by lithium chloride reduced its association with TSC1 whereas disruption of GSK3-phosphorylation sites in TSC1 reduced interaction between TSC2 and TSC1. Collectively, our data provide further evidence that beta-catenin signaling plays a role in TSC pathogenesis in vivo and suggest a novel role of GSK3 in modulating the TSC1/TSC2 complex through TSC1 phosphorylation.
结节性硬化症(TSC)相关的病理学表现出多样的表型,提示多种信号通路存在异常信号传导。除了TSC1/TSC2蛋白对mTOR的负调控作用外,我们还报道了其在体外对降解复合物水平的β-连环蛋白信号传导有影响。TSC1/TSC2复合物与GSK3和Axin结合,并促进β-连环蛋白降解,以抑制Wnt刺激的TCF/LEF依赖性转录。在此,我们表明β-连环蛋白及其效应分子细胞周期蛋白D1和连接蛋白43在TSC相关的肾血管平滑肌脂肪瘤和淋巴管平滑肌瘤病中上调。三个致病的TSC2错义突变体无法抑制Wnt信号传导,支持了这一观点。此外,TSC1/TSC2与β-连环蛋白降解复合物各组分之间的相互作用依赖于Wnt刺激,使得在有Wnt存在的情况下,结节蛋白与GSK3和Axin的结合减少,而结节蛋白与Dishevelled的相互作用增加。GSK3活性在调节降解复合物的组装/稳定性中发挥作用。氯化锂对GSK3的抑制降低了其与TSC1的结合,而TSC1中GSK3磷酸化位点的破坏减少了TSC2与TSC1之间的相互作用。总体而言,我们的数据进一步证明β-连环蛋白信号传导在TSC体内发病机制中起作用,并提示GSK3通过TSC1磷酸化调节TSC1/TSC2复合物的新作用。