Boulon Richard, Mazeaud Clément, Farahani Majid D, Broquière Mathilde, Iddir Mustapha, Charpentier Tania, Anton Anaïs, Ayotte Yann, Woo Simon, Lamarre Alain, Chatel-Chaix Laurent, LaPlante Steven R
Institut National de la Recherche Scientifique-Centre Armand-Frappier Santé Biotechnologie, 531 boulevard des Prairies, Laval, Québec H7V 1B7, Canada.
NMX Research and Solutions|Accelerating drug discovery, 500 boulevard Cartier Ouest, Laval, Quebec H7V 5B7, Canada.
ACS Pharmacol Transl Sci. 2024 Nov 5;7(12):4043-4055. doi: 10.1021/acsptsci.4c00512. eCollection 2024 Dec 13.
Drug repurposing can serve an important role in rapidly discovering medicament options for emerging microbial pandemics. In this study, a pragmatic approach is demonstrated for screening and testing drug combinations as potential broad-spectrum therapies against SARS-CoV-2 and other betacoronaviruses. Rapid cell-based phenotypic small molecule screens were executed using related common-cold-causing HCoV-OC43 betacoronavirus to identify replication inhibitors from a library of drugs approved by regulatory agencies for other indications. Given the best inhibitors, an expedient checkerboard strategy then served to identify synergistic drug combinations. These combinations were then validated using more challenging assays involving SARS-CoV-2 and variants. Promising drug combinations against multiple viral variants were discovered and involved Tilorone with Nelfinavir or Molnupiravir.
药物重新利用在迅速发现应对新出现的微生物大流行的药物选择方面可以发挥重要作用。在本研究中,展示了一种实用方法,用于筛选和测试药物组合,作为针对严重急性呼吸综合征冠状病毒2(SARS-CoV-2)和其他β冠状病毒的潜在广谱疗法。使用引起普通感冒的相关HCoV-OC43β冠状病毒进行基于细胞的快速表型小分子筛选,以从监管机构批准用于其他适应症的药物库中识别复制抑制剂。鉴于最佳抑制剂,一种便捷的棋盘策略随后用于识别协同药物组合。然后使用涉及SARS-CoV-2及其变体的更具挑战性的试验对这些组合进行验证。发现了针对多种病毒变体的有前景的药物组合,包括泰洛龙与奈非那韦或莫努匹拉韦。