Geometric Deep Learning for Structure-Based Drug Design: A Survey

Fuente: arXiv
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Main Authors: Zhang, Zaixi, Yan, Jiaxian, Huang, Yining, Liu, Qi, Chen, Enhong, Wang, Mengdi, Zitnik, Marinka
Format: Preprint
Published: 2023
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author Zhang, Zaixi
Yan, Jiaxian
Huang, Yining
Liu, Qi
Chen, Enhong
Wang, Mengdi
Zitnik, Marinka
author_facet Zhang, Zaixi
Yan, Jiaxian
Huang, Yining
Liu, Qi
Chen, Enhong
Wang, Mengdi
Zitnik, Marinka
contents Structure-based drug design (SBDD) leverages the three-dimensional geometry of proteins to identify potential drug candidates. Traditional approaches, rooted in physicochemical modeling and domain expertise, are often resource-intensive. Recent advancements in geometric deep learning, which effectively integrate and process 3D geometric data, alongside breakthroughs in accurate protein structure predictions from tools like AlphaFold, have significantly propelled the field forward. This paper systematically reviews the state-of-the-art in geometric deep learning for SBDD. We begin by outlining foundational tasks in SBDD, discussing prevalent 3D protein representations, and highlighting representative predictive and generative models. Next, we provide an in-depth review of key tasks, including binding site prediction, binding pose generation, de novo molecule generation, linker design, protein pocket generation, and binding affinity prediction. For each task, we present formal problem definitions, key methods, datasets, evaluation metrics, and performance benchmarks. Lastly, we explore current challenges and future opportunities in SBDD. Challenges include oversimplified problem formulations, limited out-of-distribution generalization, biosecurity concerns related to the misuse of structural data, insufficient evaluation metrics and large-scale benchmarks, and the need for experimental validation and enhanced model interpretability. Opportunities lie in leveraging multimodal datasets, integrating domain knowledge, developing comprehensive benchmarks, establishing criteria aligned with clinical outcomes, and designing foundation models to expand the scope of design tasks. We also curate \url{https://github.com/zaixizhang/Awesome-SBDD}, reflecting ongoing contributions and new datasets in SBDD.
format Preprint
id arxiv_https___arxiv_org_abs_2306_11768
institution arXiv
publishDate 2023
record_format arxiv
spellingShingle Geometric Deep Learning for Structure-Based Drug Design: A Survey
Zhang, Zaixi
Yan, Jiaxian
Huang, Yining
Liu, Qi
Chen, Enhong
Wang, Mengdi
Zitnik, Marinka
Quantitative Methods
Computational Engineering, Finance, and Science
Machine Learning
Structure-based drug design (SBDD) leverages the three-dimensional geometry of proteins to identify potential drug candidates. Traditional approaches, rooted in physicochemical modeling and domain expertise, are often resource-intensive. Recent advancements in geometric deep learning, which effectively integrate and process 3D geometric data, alongside breakthroughs in accurate protein structure predictions from tools like AlphaFold, have significantly propelled the field forward. This paper systematically reviews the state-of-the-art in geometric deep learning for SBDD. We begin by outlining foundational tasks in SBDD, discussing prevalent 3D protein representations, and highlighting representative predictive and generative models. Next, we provide an in-depth review of key tasks, including binding site prediction, binding pose generation, de novo molecule generation, linker design, protein pocket generation, and binding affinity prediction. For each task, we present formal problem definitions, key methods, datasets, evaluation metrics, and performance benchmarks. Lastly, we explore current challenges and future opportunities in SBDD. Challenges include oversimplified problem formulations, limited out-of-distribution generalization, biosecurity concerns related to the misuse of structural data, insufficient evaluation metrics and large-scale benchmarks, and the need for experimental validation and enhanced model interpretability. Opportunities lie in leveraging multimodal datasets, integrating domain knowledge, developing comprehensive benchmarks, establishing criteria aligned with clinical outcomes, and designing foundation models to expand the scope of design tasks. We also curate \url{https://github.com/zaixizhang/Awesome-SBDD}, reflecting ongoing contributions and new datasets in SBDD.
title Geometric Deep Learning for Structure-Based Drug Design: A Survey
topic Quantitative Methods
Computational Engineering, Finance, and Science
Machine Learning
url https://arxiv.org/abs/2306.11768