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抗精神病药/抗神经精神药物中小分子 PARKIN 激活剂的发现:一种治疗 PD 的计算机药物再利用方法。

Discovery of Small Molecule PARKIN Activator from Antipsychotic/Anti-neuropsychiatric Drugs as Therapeutics for PD: an In Silico Repurposing Approach.

机构信息

Drosophila Laboratory, Department of Biochemistry, University of Ibadan, Ibadan, Oyo State, Nigeria.

Department of Biochemistry and Molecular Biology, Usmanu Danfodiyo University, Sokoto, Nigeria.

出版信息

Appl Biochem Biotechnol. 2023 Oct;195(10):5980-6002. doi: 10.1007/s12010-023-04376-2. Epub 2023 Feb 3.

DOI:10.1007/s12010-023-04376-2
PMID:36735144
Abstract

Although there is presently no cure for Parkinson's disease (PD), the available therapies are only able to lessen symptoms and preserve the quality of life. Around 10 million people globally had PD as of 2020. The widely used standard drug has recently been revealed to have several negative effects. Additionally, there is a dearth of innovative compounds entering the market as a result of subpar ADMET characteristics. Drug repurposing provides a chance to reenergize the sluggish drug discovery process by identifying new applications for already-approved medications. As this strategy offers a practical way to speed up the process of developing alternative medications for PD. This study used a computer-aided technique to select therapeutic agent(s) from FDA-approved neuropsychiatric/psychotic drugs that can be adopted in the treatment of Parkinson's disease. In the current work, a computational approach via molecular docking, density functional theory (DFT), and pharmacokinetics were used to identify possible (anti)neuropsychiatric/psychotic medications for the treatment of PD. By using molecular docking, about eight (anti)neuropsychiatric/psychotic medications were tested against PARKIN, a key protein in PD. Based on the docking score, the best ligand in the trial was determined. The top hits were compared to the reference ligand levodopa (L-DOPA). A large proportion of the drugs displayed binding affinity that was relatively higher than L-DOPA. Also, DFT analysis confirms the ligand-receptor interactions and the molecular charge transfer. All the compounds were found to obey Lipinski's rule with acceptable pharmacokinetic properties. The current study has revealed the effectiveness of antineuropsychiatric/antipsychotic drugs against PARKIN in the treatment of PD and lumateperone was revealed to be the most promising candidate interacting with PARKIN.

摘要

虽然目前尚无治愈帕金森病(PD)的方法,但现有疗法只能减轻症状并维持生活质量。截至 2020 年,全球约有 1000 万人患有 PD。最近发现,广泛使用的标准药物有多种副作用。此外,由于 ADMET 特性不佳,进入市场的创新化合物稀缺。药物再利用为识别已批准药物的新用途,为缓慢的药物发现过程提供了重新注入活力的机会。由于这种策略为寻找治疗 PD 的替代药物提供了实用的方法,因此可以加快这一过程。本研究使用计算机辅助技术从已批准的神经精神/精神病药物中选择治疗剂,以治疗帕金森病。在目前的工作中,通过分子对接、密度泛函理论(DFT)和药代动力学的计算方法,确定了可能用于治疗 PD 的(抗)神经精神/精神病药物。通过分子对接,大约八种(抗)神经精神/精神病药物针对 PD 中的关键蛋白 PARKIN 进行了测试。根据对接评分,确定了试验中的最佳配体。将最佳配体与参考配体左旋多巴(L-DOPA)进行了比较。大部分药物显示出的结合亲和力相对高于 L-DOPA。此外,DFT 分析证实了配体-受体相互作用和分子电荷转移。所有化合物均符合 Lipinski 规则,具有可接受的药代动力学特性。本研究揭示了抗神经精神/抗精神病药物对 PD 中 PARKIN 的治疗效果,并且发现lumateperone 与 PARKIN 相互作用最有前途。

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