Wang Yi, Chen Xiushan
Chinese Materia Medica Pharmacology, Shandong Academy of Chinese Medicine, Jinan, 250014 China.
College of Chemistry and Chemical Engineering, China University of Petroleum, Qingdao, 266580 China.
In Silico Pharmacol. 2025 Jan 7;13(1):11. doi: 10.1007/s40203-024-00299-w. eCollection 2025.
Matrix metalloproteinase-8 (MMP-8), a type II collagenase, is a key enzyme in the degradation of collagens and is implicated in various pathological processes, making it a promising target for drug discovery. Despite advancements in the development of MMP-8 inhibitors, concerns over potential adverse effects persist. This study aims to address these concerns by focusing on the development of novel compounds with improved safety profiles while maintaining efficacy. In this study, we employed a computational approach to screen potent and safe inhibitors of MMP-8 from the Natural Product Activity and Species Source Database (NPASS). Initially, we constructed a pharmacophore model based on the crystal structure of the MMP-8-FIN complex (PDB ID: 4EY6) utilizing the Pharmit tool. This model then guided the selection of 44 promising molecules from NPASS, setting the stage for further analysis and evaluation. We comprehensively evaluated their drug-likeness and toxicity profiles. Molecules 21, 4, and 44 were identified as potentially effective MMP-8 inhibitors through a robust pipeline that included ADMET profiling, molecular docking, and molecular dynamics simulations. Notably, molecule 21 stood out for its low toxicity, high binding stability, and favorable ADMET profile, while molecule 44 demonstrated excellent affinity. These compounds offer structural novelty compared to known MMP-8 inhibitors. These computational results can be combined with in vitro experiments in the future to validate their activity and safety. These findings provide an important reference for drug design of MMP-8 inhibitors.
基质金属蛋白酶-8(MMP-8)是一种II型胶原酶,是胶原蛋白降解的关键酶,参与多种病理过程,使其成为药物研发的一个有前景的靶点。尽管MMP-8抑制剂的研发取得了进展,但对潜在不良反应的担忧依然存在。本研究旨在通过专注于开发具有改善安全性且保持疗效的新型化合物来解决这些担忧。在本研究中,我们采用计算方法从天然产物活性和物种来源数据库(NPASS)中筛选MMP-8的强效且安全的抑制剂。最初,我们利用Pharmit工具基于MMP-8-FIN复合物的晶体结构(PDB ID:4EY6)构建了一个药效团模型。该模型随后指导从NPASS中选择了44个有前景的分子,为进一步的分析和评估奠定了基础。我们全面评估了它们的类药性和毒性特征。通过包括ADMET分析、分子对接和分子动力学模拟在内的强大流程,确定分子21、4和44为潜在有效的MMP-8抑制剂。值得注意的是,分子21因其低毒性、高结合稳定性和良好的ADMET特征而脱颖而出,而分子44表现出优异的亲和力。与已知的MMP-8抑制剂相比,这些化合物具有结构新颖性。这些计算结果未来可与体外实验相结合,以验证它们的活性和安全性。这些发现为MMP-8抑制剂的药物设计提供了重要参考。