Division of Medicinal Chemistry, College of Pharmacy, The University of Texas at Austin, Austin, Texas 78712, United States.
Biochemistry. 2012 Nov 20;51(46):9420-35. doi: 10.1021/bi3010686. Epub 2012 Nov 8.
The bacterial degradation of the nematicide 1,3-dichloropropene, an isomeric mixture, requires the action of trans- and cis-3-chloroacrylic acid dehalogenase (CaaD and cis-CaaD, respectively). Both enzymes are tautomerase superfamily members and share a core catalytic mechanism for the hydrolytic dehalogenation of the respective isomer of 3-haloacrylate. The observation that cis-CaaD requires two additional residues raises the question of how CaaD conducts a comparable reaction with fewer catalytic residues. As part of an effort to determine the basis for the apparently simpler CaaD-catalyzed reaction, the kinetic mechanism was determined by stopped-flow and chemical-quench techniques using a fluorescent mutant form of the enzyme, αY60W-CaaD, and trans-3-bromoacrylate as the substrate. The data from these experiments as well as bromide inhibition studies are best accommodated by a six-step model that provides individual rate constants for substrate binding, chemistry, and a proposed conformational change occurring after chemistry followed by release of malonate semialdehyde and bromide. The conformational change and product release rates are comparable, and together they limit the rate of turnover. The kinetic analysis and modeling studies validate the αY60W-CaaD mutant as an accurate reporter of active site events during the course of the enzyme-catalyzed reaction. The kinetic mechanism for the αY60W-CaaD-catalyzed reaction is comparable to that obtained for the cis-CaaD-catalyzed reaction. The kinetic model and the validated αY60W-CaaD mutant set the stage for an analysis of active site mutants to explore the contributions of individual catalytic residues and the basis for the simplicity of the reaction.
需利用反式和顺式 3-氯丙烯酸脱卤酶(分别为 CaaD 和 cis-CaaD)来实现对杀线虫剂 1,3-二氯丙烯的细菌降解,这两种酶均属于互变异构酶超家族成员,拥有各自 3-卤代丙烯酸异构体水解脱卤反应的核心催化机制。cis-CaaD 需要两个额外残基的这一观察结果引发了一个问题,即 CaaD 如何利用较少的催化残基进行类似的反应。作为确定 CaaD 催化反应明显更简单的基础的努力的一部分,使用酶的荧光突变体形式 αY60W-CaaD 和反式 3-溴代丙烯作为底物,通过停流和化学猝灭技术确定了动力学机制。这些实验数据以及溴化物抑制研究的结果最好通过一个六步模型来解释,该模型为底物结合、化学和化学后发生的提议构象变化提供了单独的速率常数,随后是丙二酸盐半醛和溴化物的释放。构象变化和产物释放速率相当,它们共同限制了周转率。动力学分析和建模研究验证了 αY60W-CaaD 突变体作为酶催化反应过程中活性位点事件的准确报告者。αY60W-CaaD 催化反应的动力学机制与 cis-CaaD 催化反应获得的机制相当。动力学模型和经过验证的 αY60W-CaaD 突变体为分析活性位点突变体奠定了基础,以探索单个催化残基的贡献以及反应简单性的基础。