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Structure-based drug design (SBDD), which maps target proteins to candidate molecular ligands, is a fundamental task in drug discovery. Effectively aligning protein structural representations with molecular representations, and ensuring…

Artificial Intelligence · Computer Science 2025-11-03 Wei Zhang , Zekun Guo , Yingce Xia , Peiran Jin , Shufang Xie , Tao Qin , Xiang-Yang Li

Structure-based drug design (SBDD), aiming to generate 3D molecules with high binding affinity toward target proteins, is a vital approach in novel drug discovery. Although recent generative models have shown great potential, they suffer…

Machine Learning · Computer Science 2025-11-05 Jingyuan Zhou , Hao Qian , Shikui Tu , Lei Xu

Deep generative models have achieved tremendous success in structure-based drug design in recent years, especially for generating 3D ligand molecules that bind to specific protein pocket. Notably, diffusion models have transformed ligand…

Machine Learning · Computer Science 2024-12-03 Daiheng Zhang , Chengyue Gong , Qiang Liu

Motivation: Structure-based drug design (SBDD) has advanced with deep generative models, but bridging the gap between continuous atomic coordinates and discrete atom types remains a challenge. Current approaches, such as diffusion and flow…

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

Designing biological sequences that satisfy multiple, often conflicting, functional and biophysical criteria remains a central challenge in biomolecule engineering. While discrete flow matching models have recently shown promise for…

Machine Learning · Computer Science 2025-05-15 Tong Chen , Yinuo Zhang , Sophia Tang , Pranam Chatterjee

Structure-based drug design (SBDD), which aims to generate molecules that can bind tightly to the target protein, is an essential problem in drug discovery, and previous approaches have achieved initial success. However, most existing…

Machine Learning · Computer Science 2024-04-04 Xinze Li , Penglei Wang , Tianfan Fu , Wenhao Gao , Chengtao Li , Leilei Shi , Junhong Liu

Diffusion models have achieved promising results for Structure-Based Drug Design (SBDD). Nevertheless, high-quality protein subpocket and ligand data are relatively scarce, which hinders the models' generation capabilities. Recently, Direct…

Biomolecules · Quantitative Biology 2026-02-11 Xiwei Cheng , Xiangxin Zhou , Yuwei Yang , Yu Bao , Quanquan Gu

Structure-Based molecule optimization (SBMO) aims to optimize molecules with both continuous coordinates and discrete types against protein targets. A promising direction is to exert gradient guidance on generative models given its…

Biomolecules · Quantitative Biology 2025-06-06 Keyue Qiu , Yuxuan Song , Jie Yu , Hongbo Ma , Ziyao Cao , Zhilong Zhang , Yushuai Wu , Mingyue Zheng , Hao Zhou , Wei-Ying Ma

Generating ligand molecules for specific protein targets, known as structure-based drug design, is a fundamental problem in therapeutics development and biological discovery. Recently, target-aware generative models, especially diffusion…

Biomolecules · Quantitative Biology 2024-10-29 Siyi Gu , Minkai Xu , Alexander Powers , Weili Nie , Tomas Geffner , Karsten Kreis , Jure Leskovec , Arash Vahdat , Stefano Ermon

Recent advancements in biology and chemistry have leveraged multi-modal learning, integrating molecules and their natural language descriptions to enhance drug discovery. However, current pre-training frameworks are limited to two…

Machine Learning · Computer Science 2025-02-05 Teng Xiao , Chao Cui , Huaisheng Zhu , Vasant G. Honavar

Deep generative models provide a promising approach to de novo 3D peptide design. Most of them jointly model the distributions of peptide's position, orientation, and conformation, attempting to simultaneously converge to the target pocket.…

Quantitative Methods · Quantitative Biology 2025-11-04 Dengdeng Huang , Shikui Tu

Structure-based drug design aims at generating high affinity ligands with prior knowledge of 3D target structures. Existing methods either use conditional generative model to learn the distribution of 3D ligands given target binding sites,…

Biomolecules · Quantitative Biology 2024-03-18 Yuwei Yang , Siqi Ouyang , Xueyu Hu , Mingyue Zheng , Hao Zhou , Lei Li

Structure-Based Drug Design (SBDD) is crucial for identifying bioactive molecules. Recent deep generative models are faced with challenges in geometric structure modeling. A major bottleneck lies in the twisted probability path of…

Biomolecules · Quantitative Biology 2025-06-06 Keyue Qiu , Yuxuan Song , Zhehuan Fan , Peidong Liu , Zhe Zhang , Mingyue Zheng , Hao Zhou , Wei-Ying Ma

We introduce DrugFlow, a generative model for structure-based drug design that integrates continuous flow matching with discrete Markov bridges, demonstrating state-of-the-art performance in learning chemical, geometric, and physical…

Machine Learning · Computer Science 2025-08-26 Arne Schneuing , Ilia Igashov , Adrian W. Dobbelstein , Thomas Castiglione , Michael Bronstein , Bruno Correia

Powerful generative AI models of protein-ligand structure have recently been proposed, but few of these methods support both flexible protein-ligand docking and affinity estimation. Of those that do, none can directly model multiple binding…

Machine Learning · Computer Science 2025-03-25 Alex Morehead , Jianlin Cheng

Structure-based drug design (SBDD) is a critical task in drug discovery, requiring the generation of molecular information across two distinct modalities: discrete molecular graphs and continuous 3D coordinates. However, existing SBDD…

Computational Engineering, Finance, and Science · Computer Science 2025-03-28 Xiuyuan Hu , Guoqing Liu , Can Chen , Yang Zhao , Hao Zhang , Xue Liu

Designing molecules with desirable physiochemical properties and functionalities is a long-standing challenge in chemistry, material science, and drug discovery. Recently, machine learning-based generative models have emerged as promising…

Biomolecules · Quantitative Biology 2023-04-26 Zaixi Zhang , Qi Liu , Chee-Kong Lee , Chang-Yu Hsieh , Enhong Chen

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

Recent advances in language models have enabled framing molecule generation as sequence modeling. However, existing approaches often rely on single-objective reinforcement learning, limiting their applicability to real-world drug design,…

Machine Learning · Computer Science 2025-02-11 Diego Calanzone , Pierluca D'Oro , Pierre-Luc Bacon
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