Agrawal Nikhil, Parisini Emilio
Latvian Institute of Organic Synthesis, Aizkraukles 21, LV, Riga 1006, Latvia.
College of Health Sciences, University of KwaZulu-Natal, Durban, South Africa.
Comput Struct Biotechnol J. 2022 Sep 3;20:4892-4901. doi: 10.1016/j.csbj.2022.08.060. eCollection 2022.
PAP248-286 peptides, which are highly abundant in human semen, aggregate and form amyloid fibrils that enhance HIV infection. Previous experimental studies have shown that the infection-promoting activity of PAP248-286 begins to increase well before amyloid formation takes place and that pH plays a key role in the enhancement of PAP248-286-related infection. Hence, understanding the early stages of misfolding of the PAP2482-86 peptide is crucial. To this end, we have performed 60 independent MD simulations for a total of 24 µs at two different pH values (4.2 and 7.2). Our data shows that early stages of misfolding of the PAP248-286 peptide is a multistage process and that the first step of the process is a transition from an "I-shaped" structure to a "U-shaped" structure. We further observed that the structure of PAP248-286 at the two different pH values shows significantly different features. At pH 4.2, the peptide has less intra-molecular H-bonds and a reduced α-helical content than at pH 7.2. Moreover, differences in intra-peptide residues contacts are also observed at the two pH values. Finally, free energy landscape analysis shows that there are more local minima in the energy surface of the peptide at pH 7.2 than at pH 4.2. Overall, the present study elucidates the early stages of misfolding of the PAP248-286 peptide at the atomic level, thus possibly opening new avenues in structure-based drug discovery against HIV infection.
PAP248 - 286肽在人类精液中含量极高,会聚集并形成淀粉样纤维,从而增强HIV感染。先前的实验研究表明,PAP248 - 286促进感染的活性在淀粉样形成之前就开始显著增加,并且pH值在增强PAP248 - 286相关感染中起关键作用。因此,了解PAP248 - 286肽错误折叠的早期阶段至关重要。为此,我们在两个不同的pH值(4.2和7.2)下进行了60次独立的分子动力学模拟,总时长为24微秒。我们的数据表明,PAP248 - 286肽错误折叠的早期阶段是一个多阶段过程,该过程的第一步是从“ I形”结构转变为“ U形”结构。我们进一步观察到,PAP248 - 286在两个不同pH值下的结构显示出明显不同的特征。在pH 4.2时,该肽的分子内氢键比在pH 7.2时少,α - 螺旋含量也降低。此外,在两个pH值下还观察到肽内残基接触的差异。最后,自由能景观分析表明,pH 7.2时肽的能量表面比pH 4.2时有更多的局部最小值。总体而言,本研究在原子水平上阐明了PAP248 - 286肽错误折叠的早期阶段,从而可能为基于结构的抗HIV感染药物发现开辟新途径。