Alrouji Mohammed, Alhumaydhi Fahad A, Al Abdulmonem Waleed, Sharaf Sharaf E, Shahwan Moyad, Majarisi Taghreed, Atiya Akhtar, Shamsi Anas
Department of Medical Laboratories, College of Applied Medical Sciences, Shaqra University, 11961, Shaqra, Saudi Arabia.
Department of Medical Laboratories, College of Applied Medical Sciences, Qassim University, 52571, Buraydah, Saudi Arabia.
Mol Divers. 2024 Oct;28(5):2967-2980. doi: 10.1007/s11030-023-10726-3. Epub 2023 Sep 20.
β-secretase 1 (BACE1) is an enzyme that is involved in generating beta-amyloid peptides and is believed to have a significant role in the development of Alzheimer's disease (AD). Therefore, BACE1 has gained attention as a potential therapeutic target for treating AD. Modern drug discovery studies are being conducted to identify potential inhibitors of BACE1, with the goal of reducing the production of beta-amyloid peptides and, thus, slowing the progression of AD. Here, we used a multistep virtual screening methodology to identify phytoconstituents from the IMPPAT library that could inhibit the activity of BACE1. Molecular docking was employed to select initial hits based on their binding affinity toward BACE1. Screening for PAINS patterns, ADMET and PASS properties, was then used to identify potential molecules for BACE1 inhibition. In the end, we discovered two natural compounds, Peiminine and 27-Deoxywithaferin A, which demonstrated a strong affinity, effectiveness, and specific interactions for the BACE1-active site. The elucidated molecules also displayed drug likeliness. A 200 ns molecular dynamics (MD) simulation was conducted to investigate the interaction mechanism, complex stability, and conformational dynamics of BACE1 with Peiminine and 27-Deoxywithaferin A. The MD simulations demonstrated that BACE1 was stable during the simulation with Peiminine and 27-Deoxywithaferin A. Overall, the results suggested that Peiminine and 27-Deoxywithaferin A hold significant potential as scaffolds in drug development efforts targeting BACE1 for the purpose of treating AD.
β-分泌酶1(BACE1)是一种参与生成β-淀粉样肽的酶,被认为在阿尔茨海默病(AD)的发展中起重要作用。因此,BACE1作为治疗AD的潜在治疗靶点而受到关注。目前正在进行现代药物发现研究,以确定BACE1的潜在抑制剂,目标是减少β-淀粉样肽的产生,从而减缓AD的进展。在此,我们使用多步虚拟筛选方法从IMPPAT库中鉴定可抑制BACE1活性的植物成分。采用分子对接根据其对BACE1的结合亲和力选择初始命中物。然后通过筛选PAINS模式、ADMET和PASS性质来鉴定潜在的BACE1抑制分子。最后,我们发现了两种天然化合物,浙贝母碱和27-脱氧威替菲林A,它们对BACE1活性位点表现出很强的亲和力、有效性和特异性相互作用。所阐明的分子也显示出药物相似性。进行了200纳秒的分子动力学(MD)模拟,以研究BACE1与浙贝母碱和27-脱氧威替菲林A的相互作用机制、复合物稳定性和构象动力学。MD模拟表明,在与浙贝母碱和27-脱氧威替菲林A的模拟过程中,BACE1是稳定的。总体而言,结果表明浙贝母碱和27-脱氧威替菲林A在以治疗AD为目的靶向BACE1的药物开发工作中具有作为支架的巨大潜力。