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基于 DAT、SERT 和 NET 为基础的相互作用网络的可卡因成瘾的机器学习分析。

Machine Learning Analysis of Cocaine Addiction Informed by DAT, SERT, and NET-Based Interactome Networks.

机构信息

Department of Mathematics, Michigan State University, East Lansing, Michigan 48824, United States.

Department of Physiology, Michigan State University, East Lansing, Michigan 48824, United States.

出版信息

J Chem Theory Comput. 2022 Apr 12;18(4):2703-2719. doi: 10.1021/acs.jctc.2c00002. Epub 2022 Mar 16.

Abstract

Cocaine addiction is a psychosocial disorder induced by the chronic use of cocaine and causes a large number of deaths around the world. Despite decades of effort, no drugs have been approved by the Food and Drug Administration (FDA) for the treatment of cocaine dependence. Cocaine dependence is neurological and involves many interacting proteins in the interactome. Among them, the dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters are three major targets. Each of these targets has a large protein-protein interaction (PPI) network, which must be considered in the anticocaine addiction drug discovery. This work presents DAT, SERT, and NET interactome network-informed machine learning/deep learning (ML/DL) studies of cocaine addiction. We collected and analyzed 61 protein targets out of 460 proteins in the DAT, SERT, and NET PPI networks that have sufficiently large existing inhibitor datasets. Utilizing autoencoder (AE) and other ML/DL algorithms, including gradient boosting decision tree (GBDT) and multitask deep neural network (MT-DNN), we built predictive models for these targets with 115 407 inhibitors to predict drug repurposing potential and possible side effects. We further screened their absorption, distribution, metabolism, and excretion, and toxicity (ADMET) properties to search for leads having potential for developing treatments for cocaine addiction. Our approach offers a new systematic protocol for artificial intelligence (AI)-based anticocaine addiction lead discovery.

摘要

可卡因成瘾是一种由慢性使用可卡因引起的心理社会障碍,在全球范围内导致了大量死亡。尽管经过几十年的努力,食品和药物管理局 (FDA) 尚未批准任何药物用于治疗可卡因依赖。可卡因依赖是一种神经学疾病,涉及相互作用组中的许多相互作用蛋白。其中,多巴胺 (DAT)、血清素 (SERT) 和去甲肾上腺素 (NET) 转运蛋白是三个主要靶点。这些靶点中的每一个都有一个大型蛋白质-蛋白质相互作用 (PPI) 网络,在可卡因成瘾药物发现中必须考虑到这一点。这项工作提出了 DAT、SERT 和 NET 相互作用组网络启发式机器学习/深度学习 (ML/DL) 可卡因成瘾研究。我们从 DAT、SERT 和 NET PPI 网络中的 460 种蛋白质中收集和分析了 61 种蛋白质靶标,这些靶标具有足够大的现有抑制剂数据集。利用自动编码器 (AE) 和其他 ML/DL 算法,包括梯度提升决策树 (GBDT) 和多任务深度神经网络 (MT-DNN),我们为这些靶标构建了具有 115407 种抑制剂的预测模型,以预测药物再利用潜力和可能的副作用。我们进一步筛选了它们的吸收、分布、代谢和排泄以及毒性 (ADMET) 特性,以寻找具有开发可卡因成瘾治疗潜力的先导化合物。我们的方法为基于人工智能 (AI) 的抗可卡因成瘾先导化合物发现提供了一种新的系统方案。

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