HMAMP: Designing Highly Potent Antimicrobial Peptides Using a Hypervolume-Driven Multiobjective Deep Generative Model
Antimicrobial peptides (AMPs) have exhibited unprecedented potential as biomaterials in combating multidrug-resistant bacteria, prompting the proposal of many excellent generative models. However, the multiobjective nature of AMP discovery is often overlooked, contributing to the high attrition rate of drug candidates. Here, we propose a novel approach termed hypervolume-driven multiobjective AMP design (HMAMP), which prioritizes the simultaneous optimization of multiattribute AMPs. By synergizing reinforcement learning and a gradient descent algorithm rooted in the hypervolume maximization concept, HMAMP effectively biases generative processes and mitigates the pattern collapse issue. Comparative experiments show that HMAMP significantly outperforms state-of-the-art methods in effectiveness and diversity. A knee-based decision strategy is then employed to fast screen candidates with favorable physicochemical properties, aligning with the enhanced antimicrobial activity and reduced side effects. Molecular visualization further elucidates structural and functional properties of the AMPs. Overall, HMAMP is an effective approach to traverse large and complex exploration spaces to search for idealism-realism trade-off AMPs.
Authors
- Gary G. Yen (ORCID: https://orcid.org/0000-0001-8851-5348)
- Quan Zou (ORCID: https://orcid.org/0000-0001-6406-1142)
- Junfeng Shi (ORCID: https://orcid.org/0000-0001-7705-8866)
- Xiangxiang Zeng (ORCID: https://orcid.org/0000-0001-6201-0114)
- Xiangzheng Fu (ORCID: https://orcid.org/0000-0001-6840-2573)
- Xiucai Ye
- Dongsheng Cao (ORCID: https://orcid.org/0000-0003-3604-3785)
- Wang Li (ORCID: https://orcid.org/0000-0003-1286-4407)
- Yiping Liu (ORCID: https://orcid.org/0000-0001-7340-2551)
Institutions
- Central South University (CN)
- Hong Kong Baptist University (HK)
- University of Tsukuba (JP)
- University of Electronic Science and Technology of China (CN)
- Hunan University (CN)
- Frontier Science Foundation (CH)
- Oklahoma State University Oklahoma City (US)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2025-04-15
- DOI
- https://doi.org/10.1021/acs.jmedchem.4c03073
- Citations
- 9
- Primary Topic
- Antimicrobial Peptides and Activities
- Type
- article
- Field-Weighted Citation Impact
- 10.65
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Hunan Province