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The arc of drug discovery entails a multiparameter optimization problem spanning vast length scales. They key parameters range from solubility (angstroms) to protein-ligand binding (nanometers) to in vivo toxicity (meters). Through feature…

Explainable Graph Neural Networks (GNNs) have been developed and applied to drug-protein binding prediction to identify the key chemical structures in a drug that have active interactions with the target proteins. However, the key…

Biomolecules · Quantitative Biology 2023-09-25 Yang Wang , Zanyu Shi , Timothy Richardson , Kun Huang , Pathum Weerawarna , Yijie Wang

Protein-ligand scoring is a central component of structure-based drug design, underpinning molecular docking, virtual screening, and pose optimization. Conventional physics-based energy functions are often computationally expensive,…

Biomolecules · Quantitative Biology 2026-02-24 Zhangfan Yang , Baoyun Chen , Dong Xu , Jia Wang , Ruibin Bai , Junkai Ji , Zexuan Zhu

In recent years, machine learning has been proposed as a promising strategy to build accurate scoring functions for computational docking finalized to numerically empowered drug discovery. However, the latest studies have suggested that…

Quantitative Methods · Quantitative Biology 2023-02-17 F. Pellicani , D. Dal Ben , A. Perali , S. Pilati

Structure-Based Drug Design (SBDD) is a powerful strategy in computational drug discovery, utilizing three-dimensional protein structures to guide the design of molecules with improved binding affinity. However, capturing complex…

Machine Learning · Computer Science 2025-11-18 Long Xu , Yongcai Chen , Fengshuo Liu , Yuzhong Peng

With the development of computer-assisted techniques, research communities including biochemistry and deep learning have been devoted into the drug discovery field for over a decade. Various applications of deep learning have drawn great…

Machine Learning · Computer Science 2023-03-07 Wenhao Hu , Yingying Liu , Xuanyu Chen , Wenhao Chai , Hangyue Chen , Hongwei Wang , Gaoang Wang

Predicting accurate protein-ligand binding affinity is important in drug discovery but remains a challenge even with computationally expensive biophysics-based energy scoring methods and state-of-the-art deep learning approaches. Despite…

The field of machine learning for drug discovery is witnessing an explosion of novel methods. These methods are often benchmarked on simple physicochemical properties such as solubility or general druglikeness, which can be readily…

Virtual Screening is an essential technique in the early phases of drug discovery, aimed at identifying promising drug candidates from vast molecular libraries. Recently, ligand-based virtual screening has garnered significant attention due…

Biomolecules · Quantitative Biology 2024-11-22 Gengmo Zhou , Zhen Wang , Feng Yu , Guolin Ke , Zhewei Wei , Zhifeng Gao

Recent computational advances in the accurate prediction of protein three-dimensional (3D) structures from amino acid sequences now present a unique opportunity to decipher the interrelationships between proteins. This task entails--but is…

Biomolecules · Quantitative Biology 2020-05-19 Menuka Jaiswal , Saad Saleem , Yonghyeon Kweon , Eli J Draizen , Stella Veretnik , Cameron Mura , Philip E. Bourne

The de novo design of molecular structures using deep learning generative models introduces an encouraging solution to drug discovery in the face of the continuously increased cost of new drug development. From the generation of original…

Biomolecules · Quantitative Biology 2021-02-08 Yuemin Bian , Xiang-Qun Xie

Deep learning is catalyzing a scientific revolution fueled by big data, accessible toolkits, and powerful computational resources, impacting many fields including protein structural modeling. Protein structural modeling, such as predicting…

Biomolecules · Quantitative Biology 2020-07-17 Wenhao Gao , Sai Pooja Mahajan , Jeremias Sulam , Jeffrey J. Gray

The development of deep neural networks has improved representation learning in various domains, including textual, graph structural, and relational triple representations. This development opened the door to new relation extraction beyond…

Computation and Language · Computer Science 2022-12-22 Masaki Asada

Protein interactions are important in a broad range of biological processes. Traditionally, computational methods have been developed to automatically predict protein interface from hand-crafted features. Recent approaches employ deep…

Machine Learning · Computer Science 2020-07-21 Yi Liu , Hao Yuan , Lei Cai , Shuiwang Ji

Structure-Based Drug Design (SBDD) has revolutionized drug discovery by enabling the rational design of molecules for specific protein targets. Despite significant advancements in improving docking scores, advanced 3D-SBDD generative models…

Biomolecules · Quantitative Biology 2025-03-04 Bowen Gao , Yanwen Huang , Yiqiao Liu , Wenxuan Xie , Wei-Ying Ma , Ya-Qin Zhang , Yanyan Lan

Despite recent advances in protein-ligand structure prediction, deep learning methods remain limited in their ability to accurately predict binding affinities, particularly for novel protein targets dissimilar from the training set. In…

Quantitative Methods · Quantitative Biology 2025-12-04 Michael Brocidiacono , James Wellnitz , Konstantin I. Popov , Alexander Tropsha

Accurate prediction of drug-target interactions (DTI) is crucial for drug discovery. Recently, deep learning (DL) models for show promising performance for DTI prediction. However, these models can be difficult to use for both computer…

Machine Learning · Computer Science 2020-12-11 Kexin Huang , Tianfan Fu , Lucas Glass , Marinka Zitnik , Cao Xiao , Jimeng Sun

Virtual screening plays a critical role in modern drug discovery by enabling the identification of promising candidate molecules for experimental validation. Traditional machine learning methods such, as Support Vector Machines (SVM) and…

Machine Learning · Computer Science 2025-04-29 Radia Berreziga , Mohammed Brahimi , Khairedine Kraim , Hamid Azzoune

Significant differences in protein structures hinder the generalization of existing drug-target interaction (DTI) models, which often rely heavily on pre-learned binding principles or detailed annotations. In contrast, BioBridge designs an…

Machine Learning · Computer Science 2025-03-28 Xiaoqing Lian , Jie Zhu , Tianxu Lv , Shiyun Nie , Hang Fan , Guosheng Wu , Yunjun Ge , Lihua Li , Xiangxiang Zeng , Xiang Pan

Despite its potential for label-free particle diagnostics, holographic microscopy is limited by specialized processing methods that struggle to generalize across diverse settings. We introduce a deep learning architecture leveraging human…

Optics · Physics 2024-11-26 Shyam Kumar , Jiarong Hong