Arino Silvia, Sgueglia Gianmattia, Leone Linda, Oliva Rosario, Vecchio Pompea Del, Larrouy-Maumus Gerald, Lombardi Angela, De Simone Alfonso, Nastri Flavia
Department of Chemical Sciences, University of Napoli Federico II, via Cintia 26, Napoli, 80126, Italy.
Centre for Bacterial Resistance Biology, Department of Life Sciences, Faculty of Natural Sciences, Imperial College London, London, AZ, SW7 2, UK.
Chemistry. 2025 Sep 16;31(52):e01918. doi: 10.1002/chem.202501918. Epub 2025 Aug 13.
In this study, we report the identification of novel antimicrobial peptides (AMPs) via a machine learning-driven pipeline. Short Trp-rich peptide sequences were obtained using the HydrAMP deep learning (DL) algorithm, followed by the in silico screening for antimicrobial activity via the AMPlify DL model. Three candidates, namely AMP1, AMP2, and AMP3, were selected for synthesis and experimental validation. The antimicrobial activity was evaluated in vitro against a panel of Gram-positive and Gram-negative bacterial strains. Among them, AMP3 demonstrated the broader antibacterial spectrum. To investigate the mechanisms of action, we conducted detailed biophysical analyses of AMP3 interaction with liposomal models of bacterial membranes. The data revealed significant perturbation of membrane bilayer stability, supporting the proposed membrane-targeting activity of AMP3. Overall, our results underscore the potential of DL approaches for the accelerated discovery and mechanistic characterization of novel AMPs.
在本研究中,我们报告了通过机器学习驱动的流程鉴定新型抗菌肽(AMPs)。使用HydrAMP深度学习(DL)算法获得富含色氨酸的短肽序列,随后通过AMPlify DL模型进行抗菌活性的计算机模拟筛选。选择了三个候选物,即AMP1、AMP2和AMP3进行合成和实验验证。在体外对一组革兰氏阳性和革兰氏阴性细菌菌株评估了抗菌活性。其中,AMP3表现出更广泛的抗菌谱。为了研究作用机制,我们对AMP3与细菌膜脂质体模型的相互作用进行了详细的生物物理分析。数据显示膜双层稳定性受到显著扰动,支持了所提出的AMP3的膜靶向活性。总体而言,我们的结果强调了DL方法在加速发现新型AMPs及其作用机制表征方面的潜力。