Hu Zhiming, Liu Yijie, Huang Yonghong, Yu Peng
Xiangya School of Pharmacy, Central South University, Changsha, Hunan, 410013, China.
Curr Top Med Chem. 2025 May 29. doi: 10.2174/0115680266377310250526045137.
Experimental-driven directed evolution has achieved remarkable success in enzyme engineering. However, it relies on random mutagenesis and high-throughput screening, both of which have certain limitations, particularly the randomness of mutagenesis and the extensive screening workload that slows down the method's rapid development. In contrast, computer-aided directed evolution combines computational simulations with experimental techniques, providing an efficient and precise approach to enzyme rational design and optimization. By integrating computational tools, researchers can streamline the enzyme design process, improving the accuracy of mutations and screenings, which in turn accelerates enzyme optimization. This review comprehensively introduces the commonly used methods and applications of computer-aided directed evolution, discussing the tools and techniques frequently used in protein sequence analysis and structural analysis. It also covers computational simulation and prediction strategies such as homology modeling, molecular docking, molecular dynamics simulations, machine learning algorithms, and virtual screening. These tools play a critical role in predicting the effects of mutations on enzyme function and optimizing enzyme performance. Moreover, the review explores widely adopted semi-rational and rational design strategies in enzyme engineering, which combine computational predictions with experimental validation to effectively improve enzyme performance. Additionally, the article delves into the challenges and bottlenecks encountered in applying computational technologies in directed evolution, including issues related to computational precision, data quality, and the complexity of enzyme-substrate interactions. Despite these challenges, the future of computer-aided directed evolution holds great promise, with advancements in computational power, machine learning, and multi-omics data integration offering tremendous potential to overcome current limitations. In conclusion, this review aims to provide valuable insights for researchers in enzyme engineering, assisting them in developing new, efficient enzymes by integrating both experimental and computational approaches.
实验驱动的定向进化在酶工程领域取得了显著成功。然而,它依赖于随机诱变和高通量筛选,这两者都存在一定局限性,尤其是诱变的随机性以及大量的筛选工作,减缓了该方法的快速发展。相比之下,计算机辅助定向进化将计算模拟与实验技术相结合,为酶的合理设计和优化提供了一种高效且精确的方法。通过整合计算工具,研究人员可以简化酶的设计过程,提高突变和筛选的准确性,进而加速酶的优化。本综述全面介绍了计算机辅助定向进化的常用方法和应用,讨论了蛋白质序列分析和结构分析中常用的工具和技术。它还涵盖了诸如同源建模、分子对接、分子动力学模拟、机器学习算法和虚拟筛选等计算模拟和预测策略。这些工具在预测突变对酶功能的影响以及优化酶性能方面发挥着关键作用。此外,本综述探讨了酶工程中广泛采用的半理性和理性设计策略,这些策略将计算预测与实验验证相结合,以有效提高酶的性能。此外,本文深入探讨了在定向进化中应用计算技术时遇到的挑战和瓶颈,包括与计算精度、数据质量以及酶 - 底物相互作用复杂性相关的问题。尽管存在这些挑战,但计算机辅助定向进化的未来前景广阔,计算能力、机器学习和多组学数据整合方面的进展为克服当前局限性提供了巨大潜力。总之,本综述旨在为酶工程领域的研究人员提供有价值的见解,帮助他们通过整合实验和计算方法开发新型高效酶。