Shahwan Moyad, Prasad Pratibha, Yadav Dharmendra Kumar, Altwaijry Nojood, Khan Mohd Shahnawaz, Shamsi Anas
Center for Medical and Bio-Allied Health Sciences Research, Ajman University, Ajman, United Arab Emirates.
Department of Clinical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman, United Arab Emirates.
Front Pharmacol. 2024 Oct 9;15:1422080. doi: 10.3389/fphar.2024.1422080. eCollection 2024.
Depression and Parkinson's disease (PD) are devastating psychiatric and neurological disorders that require the development of novel therapeutic interventions. Drug repurposing targeting predefined pharmacological targets is a widely use approach in modern drug discovery. Monoamine oxidase B (MAO-B) is a critical protein implicated in Depression and PD. In this study, we undertook a systematic exploration of repurposed drugs as potential inhibitors of MAO-B. Exploring a library of 3,648 commercially available drug molecules, we conducted virtual screening using a molecular docking approach to target the MAO-B binding pocket. Two promising drug molecules, Brexpiprazole and Trifluperidol, were identified based on their exceptional binding potential and drug profiling. Subsequently, all-atom molecular dynamics (MD) simulations were performed on the MAO-B-ligand complexes for a trajectory of 300 nanoseconds (ns). Simulation results demonstrated that the binding of Brexpiprazole and Trifluperidol induced only minor structural alterations in MAO-B and showed significant stabilization throughout the simulation trajectory. Overall, the finding suggests that Brexpiprazole and Trifluperidol exhibit strong potential as repurposed inhibitors of MAO-B that might be explored further in experimental investigations for the development of targeted therapies for depression and PD.
抑郁症和帕金森病(PD)是极具破坏性的精神和神经疾病,需要开发新的治疗干预措施。针对预定义药理学靶点的药物重新利用是现代药物发现中广泛使用的方法。单胺氧化酶B(MAO - B)是一种与抑郁症和帕金森病有关的关键蛋白质。在本研究中,我们对作为MAO - B潜在抑制剂的重新利用药物进行了系统探索。通过探索一个包含3648种市售药物分子的文库,我们使用分子对接方法进行虚拟筛选,以靶向MAO - B结合口袋。基于其出色的结合潜力和药物分析,鉴定出了两种有前景的药物分子,布雷哌唑和三氟哌多。随后,对MAO - B - 配体复合物进行了全原子分子动力学(MD)模拟,模拟时长为300纳秒(ns)。模拟结果表明,布雷哌唑和三氟哌多的结合仅在MAO - B中引起轻微的结构改变,并且在整个模拟轨迹中显示出显著的稳定性。总体而言,该发现表明布雷哌唑和三氟哌多作为MAO - B的重新利用抑制剂具有强大潜力,可能在针对抑郁症和帕金森病的靶向治疗开发的实验研究中进一步探索。