SPIN:用于结合亲和力预测的 SE(3)-Invariant 物理信息网络

Seungyeon Choi, Sangmin Seo, Sanghyun Park
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引用次数: 0

摘要

准确预测蛋白质配体的结合亲和力对于快速高效地开发药物至关重要。最近,由于预测结合亲和力的重要性,利用图神经网络模拟蛋白质配体复合物的三维结构来预测结合亲和力的研究受到越来越多的关注。然而,传统方法往往无法准确模拟复合物的空间信息,或者仅仅依赖几何特征,而忽视了蛋白质配体结合的原理。这会导致过度拟合,导致模型在独立数据集上表现不佳,最终降低其在实际药物开发中的实用性。为了解决这个问题,我们提出了 SPIN 模型,该模型旨在通过结合适用于该任务的各种归纳偏差来实现卓越的泛化,而不仅仅是根据数据集的经验数据进行训练。在预测方面,我们定义了两种类型的归纳偏差:一种是从几何角度出发,无论复合物如何旋转和平移,都能保持一致的结合亲和力预测;另一种是从物理化学角度出发,为了实现蛋白质与配体的有效结合,需要将反应坐标上的结合自由能降到最低。这些先验知识输入使 SPIN 在 CASF-2016 和 CSAR HiQ 等基准集中的表现优于比较模型。此外,我们还通过虚拟筛选实验证明了我们模型的实用性,并根据评估其可解释性的实验验证了我们提出的模型的可靠性和潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
SPIN: SE(3)-Invariant Physics Informed Network for Binding Affinity Prediction
Accurate prediction of protein-ligand binding affinity is crucial for rapid and efficient drug development. Recently, the importance of predicting binding affinity has led to increased attention on research that models the three-dimensional structure of protein-ligand complexes using graph neural networks to predict binding affinity. However, traditional methods often fail to accurately model the complex's spatial information or rely solely on geometric features, neglecting the principles of protein-ligand binding. This can lead to overfitting, resulting in models that perform poorly on independent datasets and ultimately reducing their usefulness in real drug development. To address this issue, we propose SPIN, a model designed to achieve superior generalization by incorporating various inductive biases applicable to this task, beyond merely training on empirical data from datasets. For prediction, we defined two types of inductive biases: a geometric perspective that maintains consistent binding affinity predictions regardless of the complexs rotations and translations, and a physicochemical perspective that necessitates minimal binding free energy along their reaction coordinate for effective protein-ligand binding. These prior knowledge inputs enable the SPIN to outperform comparative models in benchmark sets such as CASF-2016 and CSAR HiQ. Furthermore, we demonstrated the practicality of our model through virtual screening experiments and validated the reliability and potential of our proposed model based on experiments assessing its interpretability.
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