Zhang Qi, Wei Yuxiao, Liu Liwei
College of Science, Dalian Jiaotong University, Dalian, 116028, China.
College of Software, Dalian Jiaotong University, Dalian, 116028, China.
Interdiscip Sci. 2025 Jan 7. doi: 10.1007/s12539-024-00680-5.
Accurate prediction of drug-drug interaction (DDI) is essential to improve clinical efficacy, avoid adverse effects of drug combination therapy, and enhance drug safety. Recently researchers have developed several computer-aided methods for DDI prediction. However, these methods lack the substructural features that are critical to drug interactions and are not effective in generalizing across domains and different distribution data. In this work, we present SAGAN, a domain adaptive interpretable substructure-aware graph attention network for DDI prediction. Based on attention mechanism and unsupervised clustering algorithm, we propose a new substructure segmentation method, which segments the drug molecule into multiple substructures, learns the mechanism of drug interaction from the perspective of interaction, and identifies important interaction regions between drugs. To enhance the generalization ability of the model, we improve and apply a conditional domain adversarial network to achieve cross-domain generalization by alternately optimizing the cross-entropy loss on the source domain and the adversarial loss of the domain discriminator. We evaluate and compare SAGAN with the state-of-the-art DDI prediction model on four real-world datasets for both in-domain and cross-domain scenarios, and show that SAGAN achieves the best overall performance. Moreover, the visualization results of the model show that SAGAN has achieved pharmacologically significant substructure extraction, which can help drug developers screen for some undiscovered local interaction sites, and provide important information for further drug structure optimization. The codes and datasets are available online at https://github.com/wyx2012/SAGAN .
准确预测药物相互作用(DDI)对于提高临床疗效、避免联合药物治疗的不良反应以及增强药物安全性至关重要。最近,研究人员开发了几种用于DDI预测的计算机辅助方法。然而,这些方法缺乏对药物相互作用至关重要的子结构特征,并且在跨领域和不同分布数据的泛化方面效果不佳。在这项工作中,我们提出了SAGAN,一种用于DDI预测的领域自适应可解释子结构感知图注意力网络。基于注意力机制和无监督聚类算法,我们提出了一种新的子结构分割方法,该方法将药物分子分割成多个子结构,从相互作用的角度学习药物相互作用的机制,并识别药物之间重要的相互作用区域。为了提高模型的泛化能力,我们改进并应用了条件领域对抗网络,通过交替优化源域上的交叉熵损失和领域判别器的对抗损失来实现跨领域泛化。我们在四个真实世界数据集上针对域内和跨域场景对SAGAN与最先进的DDI预测模型进行了评估和比较,结果表明SAGAN实现了最佳的整体性能。此外,模型的可视化结果表明SAGAN已经实现了具有药理学意义的子结构提取,这可以帮助药物开发者筛选一些未发现的局部相互作用位点,并为进一步的药物结构优化提供重要信息。代码和数据集可在https://github.com/wyx2012/SAGAN上在线获取。