应用深度学习预测药物的持久性、生物蓄积性和毒性

IF 5.3 2区 化学 Q1 CHEMISTRY, MEDICINAL
Dominga Evangelista, Elliot Nelson, Rachael Skyner, Ben Tehan, Mattia Bernetti, Marinella Roberti, Maria Laura Bolognesi* and Giovanni Bottegoni*, 
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引用次数: 0

摘要

本研究探讨了深度学习(DL)模型的应用,特别是通过Chemprop实现的消息传递神经网络(MPNN),以预测化合物的持久性,生物蓄积性和毒性(PBT)特征,重点是药物。我们采用了聚类策略来提供对模型性能的公平评估。通过将生成的模型应用于一组药学相关分子,我们的目标是突出潜在的PBT化学物质并提取PBT相关的子结构。这些子结构可以作为结构标志,从药物发现过程的早期阶段就提醒药物设计者注意潜在的环境问题。将这些发现纳入药物开发工作流程有望在创造更环保的候选药物方面取得重大进展,同时保持其治疗效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Application of Deep Learning to Predict the Persistence, Bioaccumulation, and Toxicity of Pharmaceuticals

This study investigates the application of a deep learning (DL) model, specifically a message-passing neural network (MPNN) implemented through Chemprop, to predict the persistence, bioaccumulation, and toxicity (PBT) characteristics of compounds, with a focus on pharmaceuticals. We employed a clustering strategy to provide a fair assessment of the model performances. By applying the generated model to a set of pharmaceutically relevant molecules, we aim to highlight potential PBT chemicals and extract PBT-relevant substructures. These substructures can serve as structural flags, alerting drug designers to potential environmental issues from the earliest stages of the drug discovery process. Incorporating these findings into pharmaceutical development workflows is expected to drive significant advancements in creating more environmentally friendly drug candidates while preserving their therapeutic efficacy.

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来源期刊
CiteScore
9.80
自引率
10.70%
发文量
529
审稿时长
1.4 months
期刊介绍: The Journal of Chemical Information and Modeling publishes papers reporting new methodology and/or important applications in the fields of chemical informatics and molecular modeling. Specific topics include the representation and computer-based searching of chemical databases, molecular modeling, computer-aided molecular design of new materials, catalysts, or ligands, development of new computational methods or efficient algorithms for chemical software, and biopharmaceutical chemistry including analyses of biological activity and other issues related to drug discovery. Astute chemists, computer scientists, and information specialists look to this monthly’s insightful research studies, programming innovations, and software reviews to keep current with advances in this integral, multidisciplinary field. As a subscriber you’ll stay abreast of database search systems, use of graph theory in chemical problems, substructure search systems, pattern recognition and clustering, analysis of chemical and physical data, molecular modeling, graphics and natural language interfaces, bibliometric and citation analysis, and synthesis design and reactions databases.
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