Division of Medicinal Chemistry, College of Pharmacy, University of Texas, Austin, TX 78712, USA.
Bioorg Chem. 2011 Feb;39(1):1-9. doi: 10.1016/j.bioorg.2010.10.001. Epub 2010 Oct 20.
The isomeric mixture of cis- and trans-1,3-dichloropropene constitutes the active component of a widely used nematocide known as Telone II®. The mixture is processed by various soil bacteria to acetaldehyde through the 1,3-dichloropropene catabolic pathway. The pathway relies on an isomer-specific hydrolytic dehalogenation reaction catalyzed by cis- or trans-3-chloroacrylic acid dehalogenase, known respectively as cis-CaaD and CaaD. Previous sequence analysis and crystallographic studies of the native and covalently modified enzymes identified Pro-1, His-28, Arg-70, Arg-73, Tyr-103, and Glu-114 as key binding and catalytic residues in cis-CaaD. Mutagenesis of these residues confirmed their importance to the dehalogenation reaction. Crystal structures of the native enzyme (2.01Å resolution) and the enzyme covalently modified at the Pro-1 nitrogen by 2-hydroxypropanoate (1.65Å resolution) are reported here. Both structures are at a resolution higher than previously reported (2.75Å and 2.1Å resolution, respectively). The conformation of the covalent adduct is strikingly different from that previously reported due to its interaction with a 7-residue loop (Thr-32 to Leu-38). The participation of another active site residue, Arg-117, in catalysis and inactivation was also examined. The implications of the combined findings for the mechanisms of catalysis and inactivation are discussed.
顺式和反式 1,3-二氯丙烯的异构体混合物构成了一种广泛使用的杀线虫剂 Telone II®的有效成分。该混合物通过各种土壤细菌通过 1,3-二氯丙烯代谢途径加工成乙醛。该途径依赖于顺式或反式 3-氯丙烯酸脱卤酶催化的异构特异性水解脱卤反应,分别称为顺式-CaaD 和 CaaD。先前对天然和共价修饰酶的序列分析和晶体学研究确定了 Pro-1、His-28、Arg-70、Arg-73、Tyr-103 和 Glu-114 为顺式-CaaD 中的关键结合和催化残基。这些残基的诱变证实了它们对脱卤反应的重要性。本文报道了天然酶(2.01Å分辨率)和酶在 Pro-1 氮上通过 2-羟基丙酸盐共价修饰(1.65Å分辨率)的晶体结构。这两种结构的分辨率都高于先前报道的(分别为 2.75Å 和 2.1Å分辨率)。由于其与 7 残基环(Thr-32 到 Leu-38)的相互作用,共价加合物的构象与以前报道的明显不同。还检查了另一个活性位点残基 Arg-117 在催化和失活中的参与。讨论了综合研究结果对催化和失活机制的影响。