Curriculum in Genetics and Molecular Biology, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America.
Department of Biology, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America.
PLoS Genet. 2018 Apr 11;14(4):e1007339. doi: 10.1371/journal.pgen.1007339. eCollection 2018 Apr.
Wnt signaling provides a paradigm for cell-cell signals that regulate embryonic development and stem cell homeostasis and are inappropriately activated in cancers. The tumor suppressors APC and Axin form the core of the multiprotein destruction complex, which targets the Wnt-effector beta-catenin for phosphorylation, ubiquitination and destruction. Based on earlier work, we hypothesize that the destruction complex is a supramolecular entity that self-assembles by Axin and APC polymerization, and that regulating assembly and stability of the destruction complex underlie its function. We tested this hypothesis in Drosophila embryos, a premier model of Wnt signaling. Combining biochemistry, genetic tools to manipulate Axin and APC2 levels, advanced imaging and molecule counting, we defined destruction complex assembly, stoichiometry, and localization in vivo, and its downregulation in response to Wnt signaling. Our findings challenge and revise current models of destruction complex function. Endogenous Axin and APC2 proteins and their antagonist Dishevelled accumulate at roughly similar levels, suggesting competition for binding may be critical. By expressing Axin:GFP at near endogenous levels we found that in the absence of Wnt signals, Axin and APC2 co-assemble into large cytoplasmic complexes containing tens to hundreds of Axin proteins. Wnt signals trigger recruitment of these to the membrane, while cytoplasmic Axin levels increase, suggesting altered assembly/disassembly. Glycogen synthase kinase3 regulates destruction complex recruitment to the membrane and release of Armadillo/beta-catenin from the destruction complex. Manipulating Axin or APC2 levels had no effect on destruction complex activity when Wnt signals were absent, but, surprisingly, had opposite effects on the destruction complex when Wnt signals were present. Elevating Axin made the complex more resistant to inactivation, while elevating APC2 levels enhanced inactivation. Our data suggest both absolute levels and the ratio of these two core components affect destruction complex function, supporting models in which competition among Axin partners determines destruction complex activity.
Wnt 信号提供了一个范例,说明细胞间信号如何调节胚胎发育和干细胞稳态,并且在癌症中不恰当地被激活。肿瘤抑制因子 APC 和 Axin 形成多蛋白破坏复合物的核心,该复合物将 Wnt 效应物β-连环蛋白靶向进行磷酸化、泛素化和破坏。基于早期的工作,我们假设破坏复合物是一个超分子实体,通过 Axin 和 APC 的聚合自我组装,调节其组装和稳定性是其功能的基础。我们在果蝇胚胎中测试了这一假设,这是 Wnt 信号的主要模型。我们结合生物化学、遗传工具来操纵 Axin 和 APC2 的水平、先进的成像和分子计数,定义了破坏复合物的组装、化学计量和体内定位,以及其对 Wnt 信号的下调。我们的发现挑战并修改了破坏复合物功能的现行模型。内源性 Axin 和 APC2 蛋白及其拮抗剂 Dishevelled 积累水平大致相似,表明结合竞争可能是关键的。通过以接近内源性水平表达 Axin:GFP,我们发现,在没有 Wnt 信号的情况下,Axin 和 APC2 共同组装成含有数十到数百个 Axin 蛋白的大细胞质复合物。Wnt 信号触发这些复合物向膜的募集,同时细胞质 Axin 水平增加,表明组装/解组装发生了改变。糖原合酶激酶 3 调节破坏复合物向膜的募集以及 Armadillo/β-连环蛋白从破坏复合物中的释放。当 Wnt 信号不存在时,操纵 Axin 或 APC2 的水平对破坏复合物的活性没有影响,但令人惊讶的是,当 Wnt 信号存在时,它们对破坏复合物有相反的影响。提高 Axin 水平使复合物更能抵抗失活,而提高 APC2 水平则增强失活。我们的数据表明,这两种核心成分的绝对水平和比例都影响破坏复合物的功能,支持这样的模型,即 Axin 伴侣之间的竞争决定了破坏复合物的活性。