Latvian Institute of Organic Synthesis, Aizkraukles 21, LV, Riga 1006, Latvia.
College of Health Sciences, University of KwaZulu-Natal, Private Bag, X54001, Durban 4000, South Africa.
J Phys Chem B. 2023 Oct 26;127(42):9095-9101. doi: 10.1021/acs.jpcb.3c05385. Epub 2023 Oct 16.
PAP248-286 is a fusogenic peptide derived from prostatic acid phosphatase, commonly found in human semen, and is known to mediate HIV fusion with cell membranes. In this study, we performed 120 independent coarse-grained molecular dynamics simulations to investigate the spontaneous binding of PAP248-286 monomers, considering both charged and neutral histidine (His) residues, to membrane bilayers composed of different lipid compositions: 100% POPC, 70% POPC-30% POPG, and 50% POPC-50% POPG. Our simulations revealed that PAP248-286 displayed spontaneous binding to the membrane, with increased binding observed in the presence of anionic lipid POPG. Specifically, in systems containing 30% and 50% POPG lipids, monomer residues, particularly in the systems containing charged histidine (His) residues, exhibited prolonged binding with the membrane. Furthermore, our simulations indicated that PAP248-286 adopted a parallel orientation with the membrane, exposing its positively charged residues to the lipid bilayer. Interestingly, systems containing charged His residues showed a higher lipid occupancy around the peptide. These findings are consistent with previous experimental data, suggesting that PAP248-286 binding is enhanced in membranes with charged His residues, resembling the conditions found in the acidic vaginal pH environment. The results of our study provide further insights into the molecular mechanisms underlying the membrane binding of PAP248-286, contributing to our understanding of its potential role in HIV fusion and infection.
PAP248-286 是一种源自前列腺酸性磷酸酶的融合肽,通常存在于人类精液中,已知能介导 HIV 与细胞膜融合。在这项研究中,我们进行了 120 次独立的粗粒化分子动力学模拟,以研究 PAP248-286 单体的自发结合,同时考虑了带电荷和不带电荷的组氨酸(His)残基与由不同脂质组成的膜双层的结合:100%POPC、70%POPC-30%POPG 和 50%POPC-50%POPG。我们的模拟结果表明,PAP248-286 自发地与膜结合,在存在阴离子脂质 POPG 时,结合增加。具体而言,在含有 30%和 50%POPG 脂质的系统中,单体残基,特别是在含有带电荷的组氨酸(His)残基的系统中,与膜的结合时间延长。此外,我们的模拟表明,PAP248-286 与膜呈平行取向,将其带正电荷的残基暴露在脂质双层中。有趣的是,含有带电荷 His 残基的系统显示肽周围的脂质占有率更高。这些发现与之前的实验数据一致,表明在带电荷 His 残基的膜中,PAP248-286 的结合增强,类似于酸性阴道 pH 环境中发现的条件。我们的研究结果为 PAP248-286 与膜结合的分子机制提供了进一步的见解,有助于我们理解其在 HIV 融合和感染中的潜在作用。