Sousa Eduardo Henrique Silva, Tuckerman Jason Robert, Gonzalez Gonzalo, Gilles-Gonzalez Marie-Alda
Department of Biochemistry, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9038, USA.
Biochemistry. 2007 May 29;46(21):6249-57. doi: 10.1021/bi7003334. Epub 2007 May 8.
Bradyrhizobium japonicum FixL is a modular oxygen sensor that directs adaptations to hypoxia by coupling the status of a heme-binding domain to a histidine-protein kinase activity. The oxygen-bound form is the "off-state". The unliganded form is the "on-state" active kinase that phosphorylates a transcription factor, FixJ. We have developed methods to optimize the kinase reactions of FixL and measure the turnover rates (kcat) for reactions catalyzed by highly inhibited states of this sensor at constant, precisely known oxygen saturations. The resulting oxygen dose-response curve shows that an in vitro system with FixL and the response regulator FixJ as its only proteins manifests such a sharp ligand response that, when the proportion of deoxy-FixL decreases less than 3-fold, the kinase activity drops over 50-fold, and by the time the deoxy-FixL declines just 8-fold, the activity is inhibited over 1100-fold. This response is entirely reversible and similar to that reported for the in vivo hypoxic induction of FixLJ-regulated genes. FixL binds oxygen noncooperatively. When complexed with FixJ, FixL is dimeric in both oxy and deoxy states. Therefore traditional models involving cooperative binding of ligand or robust allosteric regulation cannot account for the extremely nonlinear kinase response to the heme saturation. This response, however, can be explained by a form of enzyme hysteresis with the simple assumptions that (i) on association of oxygen with the heme, the kinase is rapidly switched off; (ii) after dissociation of oxygen, the kinase remains inhibited longer than the average time that it takes a deoxy-heme to encounter an oxygen molecule at most oxygen saturations.
慢生根瘤菌的FixL是一种模块化氧传感器,通过将血红素结合结构域的状态与组氨酸蛋白激酶活性相偶联来指导对缺氧的适应性变化。氧结合形式为“关闭状态”。未结合配体的形式是“开启状态”的活性激酶,可使转录因子FixJ磷酸化。我们已开发出优化FixL激酶反应的方法,并在恒定且精确已知的氧饱和度下测量该传感器高度抑制状态催化反应的周转率(kcat)。所得的氧剂量响应曲线表明,以FixL和响应调节因子FixJ作为仅有的蛋白质的体外系统表现出如此敏锐的配体响应,即当脱氧FixL的比例降低不到3倍时,激酶活性下降超过50倍,而当脱氧FixL仅下降8倍时,活性被抑制超过1100倍。这种响应是完全可逆的,并且与体内FixLJ调节基因的缺氧诱导所报道的情况相似。FixL非协同结合氧。当与FixJ复合时,FixL在氧合和脱氧状态下均为二聚体。因此,涉及配体协同结合或强大变构调节的传统模型无法解释激酶对血红素饱和度的极端非线性响应。然而,这种响应可以通过一种酶滞后形式来解释,其基于以下简单假设:(i)氧与血红素结合后,激酶迅速关闭;(ii)氧解离后,激酶保持抑制的时间长于在大多数氧饱和度下脱氧血红素遇到氧分子所需的平均时间。