Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Marzolo 5, 35131 Padova, Italy.
Int J Mol Sci. 2023 Apr 12;24(8):7119. doi: 10.3390/ijms24087119.
The latest monkeypox virus outbreak in 2022 showcased the potential threat of this viral zoonosis to public health. The lack of specific treatments against this infection and the success of viral protease inhibitors-based treatments against HIV, Hepatitis C, and SARS-CoV-2, brought the monkeypox virus I7L protease under the spotlight as a potential target for the development of specific and compelling drugs against this emerging disease. In the present work, the structure of the monkeypox virus I7L protease was modeled and thoroughly characterized through a dedicated computational study. Furthermore, structural information gathered in the first part of the study was exploited to virtually screen the DrugBank database, consisting of drugs approved by the Food and Drug Administration (FDA) and clinical-stage drug candidates, in search for readily repurposable compounds with similar binding features as TTP-6171, the only non-covalent I7L protease inhibitor reported in the literature. The virtual screening resulted in the identification of 14 potential inhibitors of the monkeypox I7L protease. Finally, based on data collected within the present work, some considerations on developing allosteric modulators of the I7L protease are reported.
2022 年最新的猴痘病毒爆发凸显了这种病毒性人畜共患病对公共卫生的潜在威胁。由于缺乏针对这种感染的特定治疗方法,以及病毒蛋白酶抑制剂在治疗 HIV、丙型肝炎和 SARS-CoV-2 方面的成功,猴痘病毒 I7L 蛋白酶成为了开发针对这种新兴疾病的特异性和有吸引力药物的潜在靶点。在本工作中,通过专门的计算研究对猴痘病毒 I7L 蛋白酶的结构进行了建模和深入表征。此外,研究第一部分收集的结构信息被用于虚拟筛选 DrugBank 数据库,该数据库包含美国食品和药物管理局 (FDA) 批准的药物和临床阶段药物候选物,以寻找具有与 TTP-6171 相似结合特征的可重新利用化合物,TTP-6171 是文献中报道的唯一非共价 I7L 蛋白酶抑制剂。虚拟筛选结果鉴定出了 14 种潜在的猴痘 I7L 蛋白酶抑制剂。最后,根据本工作中收集的数据,报告了开发 I7L 蛋白酶别构调节剂的一些考虑因素。