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基于从头分子设计发现狼疮性肾炎靶向抑制剂:维纳多评分、ADMET分析和分子动力学模拟的综合应用

Discovery of lupus nephritis targeted inhibitors based on De novo molecular design: comprehensive application of vinardo scoring, ADMET analysis, and molecular dynamics simulation.

作者信息

Zhang Kaiyuan, Tang Yingkai, Yu Haiyue, Yang Jingtao, Tao Lu, Xiang Ping

机构信息

School of Clinical Medicine, Bengbu Medical College, China.

Department of Anatomy, School of basic Medicine, Bengbu Medical College, China.

出版信息

J Biomol Struct Dyn. 2024 Mar 19:1-14. doi: 10.1080/07391102.2024.2329293.

Abstract

Lupus Nephritis (LN) is an autoimmune disease affecting the kidneys, and conventional drug studies have limitations due to its imprecise and complex pathogenesis. Therefore, the aim of this study was to design a novel Lupus Nephritis-targeted drug with good clinical due potential, high potency and selectivity by computer-assisted approach.NIK belongs to the serine/threonine protein kinase, which is gaining attention as a drug target for Lupus Nephritis. we used bioinformatics, homology modelling and sequence comparison analysis, small molecule ab initio design, ADMET analysis, molecular docking, molecular dynamics simulation, and MM/PBSA analysis to design and explore the selectivity and efficiency of a novel Lupus Nephritis-targeting drug, ClImYnib, and a classical NIK inhibitor, NIK SMI1. We used bioinformatics techniques to determine the correlation between lupus nephritis and the NF-κB signaling pathway. De novo drugs design was used to create a NIK-targeted inhibitor, ClImYnib, with lower toxicity, after which we used molecular dynamics to simulate NIK SMI1 against ClImYnib, and the simulation results showed that ClImYnib had better selectivity and efficiency. Our research delves into the molecular mechanism of protein ligands, and we have designed and validated an excellent NIK inhibitor using multiple computational simulation methods. More importantly, it provides an idea of target designing small molecules.

摘要

狼疮性肾炎(LN)是一种影响肾脏的自身免疫性疾病,由于其发病机制不精确且复杂,传统的药物研究存在局限性。因此,本研究的目的是通过计算机辅助方法设计一种具有良好临床应用潜力、高效力和选择性的新型狼疮性肾炎靶向药物。NIK属于丝氨酸/苏氨酸蛋白激酶,作为狼疮性肾炎的药物靶点正受到关注。我们使用生物信息学、同源建模和序列比较分析、小分子从头设计、ADMET分析、分子对接、分子动力学模拟和MM/PBSA分析来设计和探索一种新型狼疮性肾炎靶向药物ClImYnib和一种经典的NIK抑制剂NIK SMI1的选择性和效率。我们使用生物信息学技术来确定狼疮性肾炎与NF-κB信号通路之间的相关性。利用从头药物设计创建了一种毒性较低的NIK靶向抑制剂ClImYnib,之后我们使用分子动力学模拟NIK SMI1与ClImYnib的相互作用,模拟结果表明ClImYnib具有更好的选择性和效率。我们的研究深入探讨了蛋白质配体的分子机制,并使用多种计算模拟方法设计并验证了一种优秀的NIK抑制剂。更重要的是,它为靶向设计小分子提供了思路。

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