基于聚集关注的分子构象生成的等变粗化。

IF 5.3 2区 化学 Q1 CHEMISTRY, MEDICINAL Journal of Chemical Information and Modeling Pub Date : 2025-01-13 Epub Date: 2024-12-17 DOI:10.1021/acs.jcim.4c01001
Danny Reidenbach, Aditi S Krishnapriyan
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引用次数: 0

摘要

分子构象生成(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3D结构的能力可以避免昂贵的量子力学模拟,从而加速虚拟筛选和增强结构探索。已经为MCG开发了几种生成模型,但许多模型都难以始终如一地为有意义的下游应用生产高质量的成象。为了解决这些问题,我们引入了基于扭转角的粗颗粒分子图,并将其集成到SE(3)-等变分层变分自编码器中。通过等变粗粒度,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机制从粗粒度潜在表示中恢复细粒度坐标,从而有效地生成准确的一致性。此外,我们在多个下游应用中评估了我们生成的构象的化学和生化质量,包括性质预测和大规模基于oracle的蛋白质对接。总的来说,与之前的生成模型相比,CoarsenConf生成了更准确的一致性集成。
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CoarsenConf: Equivariant Coarsening with Aggregated Attention for Molecular Conformer Generation.

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.

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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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