Department of Molecular Biology and Biochemistry, University of California Irvine, Irvine, California, United States of America.
PLoS One. 2011;6(9):e25084. doi: 10.1371/journal.pone.0025084. Epub 2011 Sep 26.
Human diseases are attributed in part to the ability of pathogens to evade the eukaryotic immune systems. A subset of these pathogens has developed mechanisms to survive in human macrophages. Yersinia pestis, the causative agent of the bubonic plague, is a predominately extracellular pathogen with the ability to survive and replicate intracellularly. A previous study has shown that a novel rip (required for intracellular proliferation) operon (ripA, ripB and ripC) is essential for replication and survival of Y. pestis in postactivated macrophages, by playing a role in lowering macrophage-produced nitric oxide (NO) levels. A bioinformatics analysis indicates that the rip operon is conserved among a distally related subset of macrophage-residing pathogens, including Burkholderia and Salmonella species, and suggests that this previously uncharacterized pathway is also required for intracellular survival of these pathogens. The focus of this study is ripA, which encodes for a protein highly homologous to 4-hydroxybutyrate-CoA transferase; however, biochemical analysis suggests that RipA functions as a butyryl-CoA transferase. The 1.9 Å X-ray crystal structure reveals that RipA belongs to the class of Family I CoA transferases and exhibits a unique tetrameric state. Molecular dynamics simulations are consistent with RipA tetramer formation and suggest a possible gating mechanism for CoA binding mediated by Val227. Together, our structural characterization and molecular dynamic simulations offer insights into acyl-CoA specificity within the active site binding pocket, and support biochemical results that RipA is a butyryl-CoA transferase. We hypothesize that the end product of the rip operon is butyrate, a known anti-inflammatory, which has been shown to lower NO levels in macrophages. Thus, the results of this molecular study of Y. pestis RipA provide a structural platform for rational inhibitor design, which may lead to a greater understanding of the role of RipA in this unique virulence pathway.
人类疾病部分归因于病原体逃避真核免疫系统的能力。其中一些病原体已经开发出在人类巨噬细胞中生存的机制。鼠疫耶尔森菌是引起腺鼠疫的病原体,主要是一种细胞外病原体,能够在细胞内生存和复制。先前的研究表明,一个新的 rip(细胞内增殖所必需)操纵子(ripA、ripB 和 ripC)对于鼠疫耶尔森菌在激活后的巨噬细胞中的复制和存活是必不可少的,因为它在降低巨噬细胞产生的一氧化氮(NO)水平方面发挥作用。生物信息学分析表明,rip 操纵子在包括伯克霍尔德菌和沙门氏菌在内的一组与巨噬细胞相关的远缘病原体中是保守的,这表明这一以前未被描述的途径对于这些病原体的细胞内生存也是必需的。本研究的重点是 ripA,它编码一种与 4-羟基丁酸-CoA 转移酶高度同源的蛋白质;然而,生化分析表明 RipA 作为丁酰-CoA 转移酶发挥作用。1.9Å X 射线晶体结构揭示 RipA 属于 I 类 CoA 转移酶家族,并表现出独特的四聚体状态。分子动力学模拟与 RipA 四聚体形成一致,并表明 CoA 结合的可能门控机制由 Val227 介导。总之,我们的结构特征和分子动力学模拟为活性位点结合口袋中的酰基-CoA 特异性提供了深入了解,并支持 RipA 是丁酰-CoA 转移酶的生化结果。我们假设 rip 操纵子的终产物是丁酸盐,一种已知的抗炎剂,它已被证明可降低巨噬细胞中的 NO 水平。因此,本研究对鼠疫耶尔森菌 RipA 的分子研究结果为合理抑制剂设计提供了一个结构平台,这可能有助于更好地理解 RipA 在这一独特毒力途径中的作用。