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Deep generative models have achieved tremendous success in designing novel drug molecules in recent years. A new thread of works have shown the great potential in advancing the specificity and success rate of in silico drug design by…

Machine Learning · Computer Science 2025-07-14 Xingang Peng , Shitong Luo , Jiaqi Guan , Qi Xie , Jian Peng , Jianzhu Ma

The advent of deep learning has introduced efficient approaches for de novo protein sequence design, significantly improving success rates and reducing development costs compared to computational or experimental methods. However, existing…

Artificial Intelligence · Computer Science 2024-07-11 Yutong Hu , Yang Tan , Andi Han , Lirong Zheng , Liang Hong , Bingxin Zhou

Drug discovery is a complex, resource-intensive process requiring significant time and cost to bring new medicines to patients. Many generative models aim to accelerate drug discovery, but few produce synthetically accessible molecules.…

Machine Learning · Computer Science 2025-01-30 Zygimantas Jocys , Zhanxing Zhu , Henriette M. G. Willems , Katayoun Farrahi

Molecular structure elucidation from spectra is a fundamental challenge in molecular science. Conventional approaches rely heavily on expert interpretation and lack scalability, while retrieval-based machine learning approaches remain…

Machine Learning · Computer Science 2025-11-06 Liang Wang , Yu Rong , Tingyang Xu , Zhenyi Zhong , Zhiyuan Liu , Pengju Wang , Deli Zhao , Qiang Liu , Shu Wu , Liang Wang , Yang Zhang

Deep generative models are rapidly advancing structure-based drug design, offering substantial promise for generating small molecule ligands that bind to specific protein targets. However, most current approaches assume a rigid protein…

Biomolecules · Quantitative Biology 2025-11-19 Xinzhe Zheng , Shiyu Jiang , Gustavo Seabra , Chenglong Li , Yanjun Li

Proteins in complex with small molecule ligands represent the core of structure-based drug discovery. However, three-dimensional representations are absent from most deep-learning-based generative models. We here present a graph-based…

Biomolecules · Quantitative Biology 2022-04-07 Seung-gu Kang , Jeffrey K. Weber , Joseph A. Morrone , Leili Zhang , Tien Huynh , Wendy D. Cornell

Recent advancements in structure-based drug design (SBDD) have significantly enhanced the efficiency and precision of drug discovery by generating molecules tailored to bind specific protein pockets. Despite these technological strides,…

Biomolecules · Quantitative Biology 2024-06-14 Bowen Gao , Haichuan Tan , Yanwen Huang , Minsi Ren , Xiao Huang , Wei-Ying Ma , Ya-Qin Zhang , Yanyan Lan

Molecular dynamics (MD) has long been the de facto choice for simulating complex atomistic systems from first principles. Recently deep learning models become a popular way to accelerate MD. Notwithstanding, existing models depend on…

Computational Engineering, Finance, and Science · Computer Science 2023-01-10 Fang Wu , Stan Z. Li

De novo molecular design has facilitated the exploration of large chemical space to accelerate drug discovery. Structure-based de novo method can overcome the data scarcity of active ligands by incorporating drug-target interaction into…

Biomolecules · Quantitative Biology 2022-09-16 Yaqin Li , Lingli Li , Yongjin Xu , Yi Yu

Artificial intelligence (AI) is increasingly used in every stage of drug development. Continuing breakthroughs in AI-based methods for drug discovery require the creation, improvement, and refinement of drug discovery data. We posit a new…

Machine Learning · Computer Science 2024-05-08 Bing Hu , Ashish Saragadam , Anita Layton , Helen Chen

Scaffold hopping is a drug discovery strategy to generate new chemical entities by modifying the core structure, the \emph{scaffold}, of a known active compound. This approach preserves the essential molecular features of the original…

Biomolecules · Quantitative Biology 2023-08-16 Jos Torge , Charles Harris , Simon V. Mathis , Pietro Lio

Structure-based drug discovery, encompassing the tasks of protein-ligand docking and pocket-aware 3D drug design, represents a core challenge in drug discovery. However, no existing work can deal with both tasks to effectively leverage the…

Computational Engineering, Finance, and Science · Computer Science 2025-02-10 Xiuyuan Hu , Guoqing Liu , Can Chen , Yang Zhao , Hao Zhang , Xue Liu

How can diffusion models process 3D geometries in a coarse-to-fine manner, akin to our multiscale view of the world? In this paper, we address the question by focusing on a fundamental biochemical problem of generating 3D molecular…

Machine Learning · Computer Science 2024-10-29 Jiwoong Park , Yang Shen

Generative AI has the potential to revolutionize drug discovery. Yet, despite recent advances in deep learning, existing models cannot generate molecules that satisfy all desired physicochemical properties. Herein, we describe IDOLpro, a…

Chemical Physics · Physics 2025-04-29 Amit Kadan , Kevin Ryczko , Erika Lloyd , Adrian Roitberg , Takeshi Yamazaki

Solving medical imaging data scarcity through semantic image generation has attracted growing attention in recent years. However, existing generative models mainly focus on synthesizing whole-organ or large-tissue structures, showing…

Image and Video Processing · Electrical Eng. & Systems 2025-12-19 Jiahao Xia , Yutao Hu , Yaolei Qi , Zhenliang Li , Wenqi Shao , Junjun He , Ying Fu , Longjiang Zhang , Guanyu Yang

Generative models for structure-based drug design (SBDD) have shown promising results in recent years. Existing works mainly focus on how to generate molecules with higher binding affinity, ignoring the feasibility prerequisites for…

Biomolecules · Quantitative Biology 2024-05-29 Yanru Qu , Keyue Qiu , Yuxuan Song , Jingjing Gong , Jiawei Han , Mingyue Zheng , Hao Zhou , Wei-Ying Ma

Generative models for structure-based molecular design hold significant promise for drug discovery, with the potential to speed up the hit-to-lead development cycle, while improving the quality of drug candidates and reducing costs. Data…

Machine Learning · Statistics 2022-04-25 Lucian Chan , Rajendra Kumar , Marcel Verdonk , Carl Poelking

Since its foundations, more than one hundred years ago, the field of structural biology has strived to understand and analyze the properties of molecules and their interactions by studying the structure that they take in 3D space. However,…

Biomolecules · Quantitative Biology 2023-02-27 Gabriele Corso

Recent advances in generative modeling, namely Diffusion models, have revolutionized generative modeling, enabling high-quality image generation tailored to user needs. This paper proposes a framework for the generative design of structural…

We introduce a framework for automatically defining and learning deep generative models with problem-specific structure. We tackle problem domains that are more traditionally solved by algorithms such as sorting, constraint satisfaction for…

Machine Learning · Computer Science 2023-06-21 Christian Weilbach , William Harvey , Frank Wood
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