Cao Sen, Zhu Cheng, Mao Qingyi, Guo Jingjing, Zhu Ning, Duan Hongliang
Faculty of Applied Sciences, Macao Polytechnic University, R. de Luís Gonzaga Gomes, Macao 999078, China.
College of Pharmaceutical Sciences, Zhejiang University of Technology, Chaowang Road, Gongshu District, Hangzhou 310014, China.
Brief Bioinform. 2025 Aug 31;26(5). doi: 10.1093/bib/bbaf488.
Cyclic peptides have emerged as a research hotspot in drug development in recent years due to their excellent stability, specificity, and cell penetration. However, existing computational models face challenges in accurately predicting the three-dimensional structures of cyclic peptides containing unnatural amino acids (unAAs), thereby limiting their drug design. The release of AlphaFold 3 has significantly enhanced the modeling capability of biomolecular complexes and enabled the inclusion of unAAs through definitions provided by the Chemical Component Dictionary (CCD). Nevertheless, its training data reliance limits its ability to accurately predict cyclic peptide structures, failing to meet the demand for precise cyclic peptide structure prediction. Based on the AlphaFold 3 framework, we developed HighFold3 by introducing the Cyclic Position Offset Encoding Matrix (CycPOEM). HighFold3 comprises two submodels: HighFold3-Linear and HighFold3-Cyclic, designed for predicting the structures of linear and cyclic peptides, respectively. Our results demonstrate that HighFold3 outperforms existing models (HighFold, HighFold2, CyclicBoltz1, NCPepFold, CABS-flex, ESMFold, and HelixFold) in cyclic peptide structure prediction. It achieves atomic-level precision in predicting cyclic peptide monomers while demonstrating enhanced accuracy and generalization capability for cyclic peptide complexes containing unAAs. This offers unprecedented technical support for the structural design and optimization of cyclic peptide-based therapeutics.
近年来,环肽因其出色的稳定性、特异性和细胞穿透性而成为药物开发中的研究热点。然而,现有的计算模型在准确预测含有非天然氨基酸(unAAs)的环肽的三维结构方面面临挑战,从而限制了它们在药物设计中的应用。AlphaFold 3的发布显著增强了生物分子复合物的建模能力,并通过化学成分字典(CCD)提供的定义实现了非天然氨基酸的纳入。尽管如此,其对训练数据的依赖限制了它准确预测环肽结构的能力,无法满足精确环肽结构预测的需求。基于AlphaFold 3框架,我们通过引入环位置偏移编码矩阵(CycPOEM)开发了HighFold3。HighFold3包含两个子模型:HighFold3-Linear和HighFold3-Cyclic,分别用于预测线性肽和环肽的结构。我们的结果表明,HighFold3在环肽结构预测方面优于现有模型(HighFold、HighFold2、CyclicBoltz1、NCPepFold、CABS-flex、ESMFold和HelixFold)。它在预测环肽单体时达到了原子级精度,同时对于含有非天然氨基酸的环肽复合物表现出更高的准确性和泛化能力。这为基于环肽的治疗药物的结构设计和优化提供了前所未有的技术支持。