DockEM:利用低至中分辨率低温电镜密度图进行原子尺度蛋白质配体对接优化的增强方法。

IF 6.8 2区 生物学 Q1 BIOCHEMICAL RESEARCH METHODS
Jing Zou, Wenyi Zhang, Jun Hu, Xiaogen Zhou, Biao Zhang
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引用次数: 0

摘要

蛋白质-配体对接在虚拟药物筛选中起着至关重要的作用,近年来低温电子显微镜(cryo-EM)技术的进步大大加快了基于结构的药物发现的进展。然而,大多数低温电镜密度图是中低分辨率的(3-10 Å),这给有效地将低温电镜数据整合到分子对接工作流程中带来了挑战。在这项研究中,我们提出了一种更新的蛋白质-配体对接方法DockEM,它利用局部低温电镜密度图和物理能量精化来精确地将配体对接到特定的蛋白质结合位点。在121个蛋白质配体化合物的数据集上测试,我们的结果表明DockEM优于其他先进的对接方法。DockEM的优势在于它能够结合低温电镜密度图信息,有效地利用这些图中嵌入的配体的结构信息。这一进步增强了低温电镜密度图在虚拟药物筛选中的应用,为药物发现提供了更可靠的框架。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
DockEM: an enhanced method for atomic-scale protein-ligand docking refinement leveraging low-to-medium resolution cryo-EM density maps.

Protein-ligand docking plays a pivotal role in virtual drug screening, and recent advancements in cryo-electron microscopy (cryo-EM) technology have significantly accelerated the progress of structure-based drug discovery. However, the majority of cryo-EM density maps are of medium to low resolution (3-10 Å), which presents challenges in effectively integrating cryo-EM data into molecular docking workflows. In this study, we present an updated protein-ligand docking method, DockEM, which leverages local cryo-EM density maps and physical energy refinement to precisely dock ligands into specific protein binding sites. Tested on a dataset of 121 protein-ligand compound, our results demonstrate that DockEM outperforms other advanced docking methods. The strength of DockEM lies in its ability to incorporate cryo-EM density map information, effectively leveraging the structural information of ligands embedded within these maps. This advancement enhances the use of cryo-EM density maps in virtual drug screening, offering a more reliable framework for drug discovery.

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来源期刊
Briefings in bioinformatics
Briefings in bioinformatics 生物-生化研究方法
CiteScore
13.20
自引率
13.70%
发文量
549
审稿时长
6 months
期刊介绍: Briefings in Bioinformatics is an international journal serving as a platform for researchers and educators in the life sciences. It also appeals to mathematicians, statisticians, and computer scientists applying their expertise to biological challenges. The journal focuses on reviews tailored for users of databases and analytical tools in contemporary genetics, molecular and systems biology. It stands out by offering practical assistance and guidance to non-specialists in computerized methodologies. Covering a wide range from introductory concepts to specific protocols and analyses, the papers address bacterial, plant, fungal, animal, and human data. The journal's detailed subject areas include genetic studies of phenotypes and genotypes, mapping, DNA sequencing, expression profiling, gene expression studies, microarrays, alignment methods, protein profiles and HMMs, lipids, metabolic and signaling pathways, structure determination and function prediction, phylogenetic studies, and education and training.
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