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Contrastive Multi-Task Learning with Solvent-Aware Augmentation for Drug Discovery
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本文介绍了一种结合溶剂条件下的配体构象集作为增强输入的预训练方法,有效预测蛋白质-配体相互作用,显著提高结合亲和力预测和虚拟筛选准确率,支持溶剂感知的多任务建模。

arXiv:2508.01799v1 Announce Type: cross Abstract: Accurate prediction of protein-ligand interactions is essential for computer-aided drug discovery. However, existing methods often fail to capture solvent-dependent conformational changes and lack the ability to jointly learn multiple related tasks. To address these limitations, we introduce a pre-training method that incorporates ligand conformational ensembles generated under diverse solvent conditions as augmented input. This design enables the model to learn both structural flexibility and environmental context in a unified manner. The training process integrates molecular reconstruction to capture local geometry, interatomic distance prediction to model spatial relationships, and contrastive learning to build solvent-invariant molecular representations. Together, these components lead to significant improvements, including a 3.7% gain in binding affinity prediction, an 82% success rate on the PoseBusters Astex docking benchmarks, and an area under the curve of 97.1% in virtual screening. The framework supports solvent-aware, multi-task modeling and produces consistent results across benchmarks. A case study further demonstrates sub-angstrom docking accuracy with a root-mean-square deviation of 0.157 angstroms, offering atomic-level insight into binding mechanisms and advancing structure-based drug design.

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药物发现 蛋白质-配体相互作用 预训练方法
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