Reidenbach Danny, Krishnapriyan Aditi S
Department of Chemical Engineering, Department of Computer Science, University of California Berkeley, Berkeley, California 94720, United States.
NVIDIA, Santa Clara, California 95051, United States.
J Chem Inf Model. 2025 Jan 13;65(1):22-30. doi: 10.1021/acs.jcim.4c01001. Epub 2024 Dec 17.
Molecular conformer generation (MCG) is an important task in cheminformatics and drug discovery. The ability to efficiently generate low-energy 3D structures can avoid expensive quantum mechanical simulations, leading to accelerated virtual screenings and enhanced structural exploration. Several generative models have been developed for MCG, but many struggle to consistently produce high-quality conformers for meaningful downstream applications. To address these issues, we introduce CoarsenConf, which coarse-grains molecular graphs based on torsional angles and integrates them into an SE(3)-equivariant hierarchical variational autoencoder. Through equivariant coarse-graining, we aggregate the fine-grained atomic coordinates of subgraphs connected via rotatable bonds, creating a variable-length coarse-grained latent representation. Our model uses a novel aggregated attention mechanism to restore fine-grained coordinates from the coarse-grained latent representation, enabling efficient generation of accurate conformers. Furthermore, we evaluate the chemical and biochemical quality of our generated conformers on multiple downstream applications, including property prediction and large-scale oracle-based protein docking. Overall, CoarsenConf generates more accurate conformer ensembles compared to prior generative models.
分子构象异构体生成(MCG)是化学信息学和药物发现中的一项重要任务。高效生成低能量三维结构的能力可以避免昂贵的量子力学模拟,从而加快虚拟筛选并增强结构探索。已经为MCG开发了几种生成模型,但许多模型难以始终为有意义的下游应用生成高质量的构象异构体。为了解决这些问题,我们引入了CoarsenConf,它基于扭转角对分子图进行粗粒度处理,并将其集成到一个SE(3)等变分层变分自编码器中。通过等变粗粒度处理,我们聚合了通过可旋转键连接的子图的细粒度原子坐标,创建了一个可变长度的粗粒度潜在表示。我们的模型使用一种新颖的聚合注意力机制从粗粒度潜在表示中恢复细粒度坐标,从而能够高效生成准确的构象异构体。此外,我们在多个下游应用中评估了我们生成的构象异构体的化学和生化质量,包括性质预测和基于大规模预言机的蛋白质对接。总体而言,与先前的生成模型相比,CoarsenConf生成了更准确的构象异构体集合。