Traverso E E, Baskerville C, Liu Y, Shou W, James P, Deshaies R J, Charbonneau H
Department of Biochemistry, Purdue University, West Lafayette, Indiana 47907, USA.
J Biol Chem. 2001 Jun 15;276(24):21924-31. doi: 10.1074/jbc.M011689200. Epub 2001 Mar 27.
In the budding yeast Saccharomyces cerevisiae, the multifunctional protein Net1 is implicated in regulating the cell cycle function of the Cdc14 protein phosphatase. Genetic and cell biological data suggest that during interphase and early mitosis Net1 holds Cdc14 within the nucleolus where its activity is suppressed. Upon its transient release from Net1 at late anaphase, active Cdc14 promotes exit from mitosis by dephosphorylating targets in the nucleus and cytoplasm. In this paper we present evidence supporting the proposed role of Net1 in regulating Cdc14 and exit from mitosis. We show that the NH(2)-terminal fragment Net1(1-600) directly binds Cdc14 in vitro and is a highly specific competitive inhibitor of its activity (K(i) = 3 nm) with five different substrates including the physiologic targets Swi5 and Sic1. An analysis of truncation mutants indicates that the Cdc14 binding site is located within a segment of Net1 containing residues 1-341. We propose that Net1 inhibits by occluding the active site of Cdc14 because it acts as a competitive inhibitor, binds to a site located within the catalytic domain (residues 1-374), binds with reduced affinity to a Cdc14 C283S mutant in which an active site Cys is replaced, and is displaced by tungstate, a transition state analog known to bind in the catalytic site of protein-tyrosine phosphatases.
在出芽酵母酿酒酵母中,多功能蛋白Net1参与调控Cdc14蛋白磷酸酶的细胞周期功能。遗传学和细胞生物学数据表明,在间期和有丝分裂早期,Net1将Cdc14滞留在核仁中,抑制其活性。在后期晚期Cdc14从Net1短暂释放后,活性Cdc14通过使细胞核和细胞质中的靶标去磷酸化来促进有丝分裂的退出。在本文中,我们提供证据支持Net1在调控Cdc14和有丝分裂退出中所提出的作用。我们表明,NH(2)末端片段Net1(1-600)在体外直接结合Cdc14,并且是其活性(K(i)=3nm)对包括生理靶标Swi5和Sic1在内的五种不同底物的高度特异性竞争性抑制剂。对截短突变体的分析表明,Cdc14结合位点位于Net1包含残基1-341的片段内。我们提出Net1通过封闭Cdc14的活性位点来抑制,因为它作为竞争性抑制剂起作用,与位于催化结构域(残基1-374)内的位点结合,与活性位点半胱氨酸被取代的Cdc14 C283S突变体的结合亲和力降低,并且被钨酸盐取代,钨酸盐是一种已知结合在蛋白酪氨酸磷酸酶催化位点的过渡态类似物。