Parkin Jamie, Khalid Syma
School of Chemistry, University of Southampton, Southampton, United Kingdom.
School of Chemistry, University of Southampton, Southampton, United Kingdom.
Biophys J. 2014 Oct 21;107(8):1853-1861. doi: 10.1016/j.bpj.2014.08.035.
Pseudomonas aeruginosa is a Gram-negative bacterium that does not contain large, nonspecific porins in its outer membrane. Consequently, the outer membrane is highly impermeable to polar solutes and serves as a barrier against the penetration of antimicrobial agents. This is one of the reasons why such bacteria are intrinsically resistant to antibiotics. Polar molecules that permeate across the outer membrane do so through substrate-specific channels proteins. To design antibiotics that target substrate-channel proteins, it is essential to first identify the permeation pathways of their natural substrates. In P. aeruginosa, the largest family of substrate-specific proteins is the OccD (previously reported under the name OprD) family. Here, we employ equilibrium and steered molecular-dynamics simulations to study OccD1/OprD, the archetypical member of the OccD family. We study the permeation of arginine, one of the natural substrates of OccD1, through the protein. The combination of simulation methods allows us to predict the pathway taken by the amino acid, which is enabled by conformational rearrangements of the extracellular loops of the protein. Furthermore, we show that arginine adopts a specific orientation to form the molecular interactions that facilitate its passage through part of the protein. We predict a three-stage permeation process for arginine.
铜绿假单胞菌是一种革兰氏阴性细菌,其外膜中不含有大型非特异性孔蛋白。因此,外膜对极性溶质具有高度不渗透性,并作为抗菌剂渗透的屏障。这是此类细菌对抗生素具有固有抗性的原因之一。穿过外膜的极性分子是通过底物特异性通道蛋白实现的。为了设计针对底物通道蛋白的抗生素,首先确定其天然底物的渗透途径至关重要。在铜绿假单胞菌中,最大的底物特异性蛋白家族是OccD(以前报道的名称为OprD)家族。在这里,我们采用平衡和引导分子动力学模拟来研究OccD家族的典型成员OccD1/OprD。我们研究了OccD1的天然底物之一精氨酸通过该蛋白的渗透过程。模拟方法的结合使我们能够预测氨基酸所采取的途径,这是由蛋白质细胞外环的构象重排实现的。此外,我们表明精氨酸采取特定的取向以形成促进其通过蛋白质部分的分子相互作用。我们预测精氨酸的渗透过程分为三个阶段。