Singh Vinay K, Pacheco Ivan, Uversky Vladimir N, Smith Steven P, MacLeod R John, Jia Zongchao
Department of Biochemistry, Queen's University, Kingston, Ontario, Canada.
J Mol Biol. 2008 Jul 4;380(2):313-26. doi: 10.1016/j.jmb.2008.04.069. Epub 2008 May 3.
Intrinsically disordered proteins are emerging as substantial functional constituents of mammalian proteomes. Although the abundance of these proteins has been established by bioinformatics approaches, the vast majority have not been characterized structurally or functionally. The C/EBP homologous protein (CHOP) is a proto-oncogene, traditionally shown as a dominant-negative inhibitor of C/EBPs and a transcriptional activator of activating protein-1. We report here the in vitro characterization of CHOP, where our computational analyses and experimental evidences show for the first time that CHOP is an intrinsically disordered protein. Intrinsic fluorescence, NMR spectroscopy, and analytical size-exclusion chromatography studies indicate that CHOP contains extensive disordered regions and self-associate in solution. Interestingly, the disordered N-terminal region has a key role in the oligomerization of CHOP and is vital for its biological activity. We report a novel mechanistic role of CHOP in the inhibition of Wnt/TCF signaling and stimulation of c-Jun and sucrase-isomaltase reporter activity in intestinal colon cancer cells. These findings are discussed in the context of oligomerization of intrinsically disordered proteins as one of the mechanisms through which they exert their biological function.
内在无序蛋白质正逐渐成为哺乳动物蛋白质组的重要功能组成部分。尽管通过生物信息学方法已确定了这些蛋白质的丰度,但绝大多数蛋白质尚未在结构或功能上得到表征。C/EBP 同源蛋白(CHOP)是一种原癌基因,传统上被认为是 C/EBP 的显性负性抑制剂和激活蛋白-1 的转录激活剂。我们在此报告 CHOP 的体外特性,我们的计算分析和实验证据首次表明 CHOP 是一种内在无序蛋白质。内在荧光、核磁共振光谱和分析型尺寸排阻色谱研究表明,CHOP 包含广泛的无序区域并在溶液中自缔合。有趣的是,无序的 N 端区域在 CHOP 的寡聚化中起关键作用,并且对其生物学活性至关重要。我们报告了 CHOP 在抑制 Wnt/TCF 信号传导以及刺激肠道结肠癌细胞中 c-Jun 和蔗糖酶-异麦芽糖酶报告基因活性方面的新机制作用。这些发现是在内在无序蛋白质寡聚化作为其发挥生物学功能的机制之一的背景下进行讨论的。