Hur Sun, Bruice Thomas C
Department of Chemistry, University of California, Santa Barbara, CA 93106, USA.
Proc Natl Acad Sci U S A. 2002 Jul 23;99(15):9668-73. doi: 10.1073/pnas.142307099. Epub 2002 Jul 9.
Molecular dynamics simulations have been used to derive the structures of ground (orotidine-5'-monophosphate decarboxylase x orotidine 5'-monophosphate; ODC x OMP) and intermediate (ODC x intermediate; ODC x I(-)) states in the ODC-catalyzed decarboxylation of OMP. For comparison, a molecular dynamics simulation of the conformers of OMP dissolved in water was also studied. This structural information is unavailable from present crystal structures. The electrostatic network in the active site around the carboxylate moiety of OMP exhibits remarkable stability. The conformation of enzyme-bound OMP is very similar to the conformation of OMP in water. Thus, the proposed Circe effect mechanism for ODC catalysis is unlikely. Comparison of ground state and intermediate state structures shows that on decarboxylation C6 takes the position of the carboxylate O8. This significant movement of the ligand is accompanied by a placement of the C6 carbanion in the vicinity of the protonated Lys-93 and is enforced by a change of the 203-218 loop from an unstructured form to an ordered beta-hairpin. Previously proposed mechanisms involving protonation at O2, O4, or C5 have in common internal stabilization of the anionic intermediate by conjugation with positive charge on the pyrimidine ring. These mechanisms are not supported because there are no proton sources near O2, O4, and C5. We propose that the stabilization of intermediate ODC x I(-) is achieved by movement of the carbanion toward the external cation Lys-93 on decarboxylation and organization of the 203-218 loop. Because the intermediate and transition state are energetically similar, stabilization of the former decreases the free energy content of the latter.
分子动力学模拟已被用于推导乳清苷-5'-单磷酸脱羧酶x乳清苷5'-单磷酸(ODC x OMP)的基态结构以及ODC催化乳清苷5'-单磷酸脱羧反应中的中间态(ODC x 中间体;ODC x I(-))结构。为作比较,还研究了溶解于水中的乳清苷5'-单磷酸构象异构体的分子动力学模拟。目前的晶体结构无法提供此结构信息。乳清苷5'-单磷酸羧酸根基团周围活性位点的静电网络表现出显著的稳定性。酶结合的乳清苷5'-单磷酸的构象与水中乳清苷5'-单磷酸的构象非常相似。因此,所提出的ODC催化的喀耳刻效应机制不太可能成立。基态和中间态结构的比较表明,脱羧时C6占据羧酸根O8的位置。配体的这一显著移动伴随着C6碳负离子置于质子化的赖氨酸-93附近,并由203 - 218环从无结构形式转变为有序的β-发夹结构所促成。先前提出的涉及O2、O4或C5质子化的机制,其共同之处在于通过与嘧啶环上的正电荷共轭来实现阴离子中间体的内部稳定。这些机制不成立,因为在O2、O4和C5附近没有质子来源。我们提出,中间体ODC x I(-)的稳定是通过脱羧时碳负离子向外部阳离子赖氨酸-93移动以及组织203 - 218环来实现的。由于中间体和过渡态在能量上相似,前者的稳定降低了后者的自由能含量。