Department of Chemistry, City College of New York , 160 Convent Avenue, New York, New York 10031, United States.
Graduate Program in Chemistry, The Graduate Center, City University of New York , 365 Fifth Avenue, New York, New York 10016, United States.
J Phys Chem B. 2017 Oct 5;121(39):9126-9140. doi: 10.1021/acs.jpcb.7b06591. Epub 2017 Sep 21.
Protegrin-1 is an 18-residue β-hairpin antimicrobial peptide (AMP) that has been suggested to form transmembrane β-barrels in biological membranes. However, alternative structures have also been proposed. Here, we performed multimicrosecond, all-atom molecular dynamics simulations of various protegrin-1 oligomers on the membrane surface and in transmembrane topologies. The membrane surface simulations indicated that protegrin dimers are stable, whereas trimers and tetramers break down. Tetrameric arcs remained stably inserted in lipid membranes, but the pore water was displaced by lipid molecules. Unsheared protegrin β-barrels opened into β-sheets that surrounded stable aqueous pores, whereas tilted barrels with sheared hydrogen bonding patterns were stable in most topologies. A third type of observed pore consisted of multiple small oligomers surrounding a small, partially lipidic pore. We also considered the β-hairpin AMP tachyplesin, which showed less tendency to oligomerize than protegrin: the octameric bundle resulted in small pores surrounded by six peptides as monomers and dimers, with some peptides returning to the membrane surface. The results imply that multiple configurations of protegrin oligomers may produce aqueous pores and illustrate the relationship between topology and putative steps in protegrin-1's pore formation. However, the long-term stability of these structures needs to be assessed further.
防御素-1 是一个由 18 个残基组成的 β-发夹抗菌肽(AMP),它被认为在生物膜中形成跨膜 β-桶状结构。然而,也提出了替代结构。在这里,我们对各种防御素-1 低聚物在膜表面和跨膜拓扑结构中的多微秒全原子分子动力学模拟进行了研究。膜表面模拟表明防御素二聚体是稳定的,而三聚体和四聚体则会分解。四聚体的弧形仍然稳定地插入脂质膜中,但孔中的水被脂质分子取代。未剪切的防御素β-桶打开成围绕稳定水孔的β-片层,而具有剪切氢键模式的倾斜桶在大多数拓扑结构中是稳定的。另一种观察到的孔由围绕小部分脂质孔的多个小低聚物组成。我们还考虑了β-发夹 AMP tachyplesin,它比防御素更不容易聚合:八聚体束形成由六个肽作为单体和二聚体包围的小孔,一些肽会回到膜表面。结果表明,防御素低聚物的多种构象可能产生水性孔,并说明了拓扑结构与防御素-1 孔形成过程中潜在步骤之间的关系。然而,这些结构的长期稳定性需要进一步评估。