Nakao Hiroyuki, Sugimoto Yuta, Ikeda Keisuke, Saito Hiroaki, Nakano Minoru
Department of Biointerface Chemistry, Faculty of Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.
Laboratory for Computational Molecular Design, RIKEN Center for Biosystems Dynamics Research, 6-2-4 Furuedai, Suita, Osaka 565-0874, Japan.
J Phys Chem Lett. 2020 Mar 5;11(5):1662-1667. doi: 10.1021/acs.jpclett.0c00175. Epub 2020 Feb 14.
Phospholipid scramblases that catalyze lipid transbilayer movement are associated with intercellular signaling and lipid homeostasis. Although several studies have shown that the hydrophilic residue-rich groove of the proteins mediates lipid scrambling, the interactions between the groove and the lipid bilayers remain poorly understood. Here we have revealed the structural features of model transmembrane peptides that conduct lipid scrambling as well as the interactions between the peptides and the surrounding lipids by means of experimental and simulation techniques. Peptides with two strongly hydrophilic residues located on the same side of the helices and at a deeper position in the membrane exhibited high scramblase activities. All-atom molecular dynamics simulations showed that the interactions between the hydrophilic residues and lipid head groups regulate the membrane thinning and disorder near the peptides in an order that correlates with the scramblase activity of the peptides. These results provide a basis for understanding the lipid scrambling mechanisms by transmembrane regions.
催化脂质跨双层运动的磷脂翻转酶与细胞间信号传导和脂质稳态相关。尽管多项研究表明,该蛋白富含亲水性残基的凹槽介导脂质翻转,但凹槽与脂质双层之间的相互作用仍知之甚少。在此,我们通过实验和模拟技术揭示了进行脂质翻转的模型跨膜肽的结构特征,以及肽与周围脂质之间的相互作用。在螺旋同一侧且位于膜内更深位置具有两个强亲水性残基的肽表现出高翻转酶活性。全原子分子动力学模拟表明,亲水性残基与脂质头部基团之间的相互作用以与肽的翻转酶活性相关的顺序调节肽附近的膜变薄和无序状态。这些结果为理解跨膜区域的脂质翻转机制提供了基础。