Cho Seunghee, Shi Ke, Seffernick Jennifer L, Dodge Anthony G, Wackett Lawrence P, Aihara Hideki
Department of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, St. Paul, Minnesota, United States of America.
Department of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, St. Paul, Minnesota, United States of America; BioTechnology Institute, University of Minnesota, St. Paul, Minnesota, United States of America.
PLoS One. 2014 Jun 10;9(6):e99349. doi: 10.1371/journal.pone.0099349. eCollection 2014.
Cyanuric acid hydrolase (CAH) catalyzes the hydrolytic ring-opening of cyanuric acid (2,4,6-trihydroxy-1,3,5-triazine), an intermediate in s-triazine bacterial degradation and a by-product from disinfection with trichloroisocyanuric acid. In the present study, an X-ray crystal structure of the CAH-barbituric acid inhibitor complex from Azorhizobium caulinodans ORS 571 has been determined at 2.7 Å resolution. The CAH protein fold consists of three structurally homologous domains forming a β-barrel-like structure with external α-helices that result in a three-fold symmetry, a dominant feature of the structure and active site that mirrors the three-fold symmetrical shape of the substrate cyanuric acid. The active site structure of CAH is similar to that of the recently determined AtzD with three pairs of active site Ser-Lys dyads. In order to determine the role of each Ser-Lys dyad in catalysis, a mutational study using a highly sensitive, enzyme-coupled assay was conducted. The 10⁹-fold loss of activity by the S226A mutant was at least ten times lower than that of the S79A and S333A mutants. In addition, bioinformatics analysis revealed the Ser226/Lys156 dyad as the only absolutely conserved dyad in the CAH/barbiturase family. These data suggest that Lys156 activates the Ser226 nucleophile which can then attack the substrate carbonyl. Our combination of structural, mutational, and bioinformatics analyses differentiates this study and provides experimental data for mechanistic insights into this unique protein family.
氰尿酸水解酶(CAH)催化氰尿酸(2,4,6 - 三羟基 - 1,3,5 - 三嗪)的水解开环反应,氰尿酸是三嗪类细菌降解过程中的中间体,也是用三氯异氰尿酸消毒产生的副产物。在本研究中,已测定了来自茎瘤固氮根瘤菌ORS 571的CAH - 巴比妥酸抑制剂复合物的X射线晶体结构,分辨率为2.7 Å。CAH蛋白折叠由三个结构同源的结构域组成,形成一个带有外部α - 螺旋的β - 桶状结构,产生三重对称性,这是该结构和活性位点的一个主要特征,反映了底物氰尿酸的三重对称形状。CAH的活性位点结构与最近确定的AtzD相似,有三对活性位点Ser - Lys二元组。为了确定每个Ser - Lys二元组在催化中的作用,使用高灵敏度的酶偶联测定法进行了突变研究。S226A突变体导致的活性丧失10⁹倍至少比S79A和S333A突变体低十倍。此外,生物信息学分析表明Ser226/Lys156二元组是CAH/巴比妥酸酶家族中唯一绝对保守的二元组。这些数据表明Lys156激活了Ser226亲核试剂,然后Ser226可以攻击底物羰基。我们结合结构、突变和生物信息学分析,使本研究具有特色,并为深入了解这个独特的蛋白质家族的机制提供了实验数据。