MultiRankDTA: A Hybrid Ranking Framework for Robust and Generalizable Drug-Target Affinity Prediction

IF 6.4 2区 化学 Q1 CHEMISTRY, MEDICINAL
Qiang Huang, Yifan Wu, Lin Wang, Jianhui Lin, Yiming Li, Min Zeng, Min Li
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引用次数: 0

Abstract

Predicting drug-target affinity (DTA) is essential for screening candidate compounds in early-stage drug discovery. However, most existing computational methods formulate DTA prediction as a regression task, leading to an objective mismatch with the practical need to rank and prioritize candidate compounds based on their relative binding strengths. Moreover, existing ranking-based methods often adopt a fixed ranking objective or scoring function, which may limit their flexibility when they are applied to diverse drug-target interaction scenarios. To address these challenges, we propose MultiRankDTA, a novel framework that formulates DTA prediction as a multilevel ranking task to better align with the practical goal of drug screening. By integrating pointwise, pairwise, and listwise ranking strategies through a mixture-of-experts (MoE) module, MultiRankDTA enables dynamic and adaptive compound prioritization. Furthermore, we introduce a fusion network to reduce data set-specific biases by leveraging auxiliary supervision from multiple sources. Extensive experiments demonstrate that MultiRankDTA achieves superior performance compared to state-of-the-art computational methods across multiple benchmark data sets and delivers strong results on an independent benchmark for virtual screening, indicating its potential for generalization and practical utility. The source code can be obtained at https://github.com/CSUBioGroup/MultiRankDTA.

MultiRankDTA:一种用于稳健通用药物靶标亲和力预测的混合排序框架
摘要预测药物靶标亲和力(DTA)是早期药物发现过程中筛选候选化合物的重要手段。然而,大多数现有的计算方法将DTA预测作为一项回归任务,导致客观不匹配基于相对结合强度对候选化合物进行排序和优先排序的实际需要。此外,现有的基于排名的方法往往采用固定的排名目标或评分函数,这限制了其在不同药物-靶点相互作用场景下的灵活性。为了解决这些挑战,我们提出了MultiRankDTA,这是一个新的框架,将DTA预测作为一个多层次的排序任务,以更好地与药物筛选的实际目标保持一致。通过专家混合(MoE)模块集成点、成对和列表排序策略,MultiRankDTA实现了动态和自适应的复合优先级。此外,我们引入了一个融合网络,通过利用来自多个来源的辅助监督来减少数据集特定的偏差。大量实验表明,与最先进的计算方法相比,MultiRankDTA在多个基准数据集上取得了卓越的性能,并在虚拟筛选的独立基准上提供了强有力的结果,表明其具有推广和实用的潜力。源代码可从https://github.com/CSUBioGroup/MultiRankDTA获得。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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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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