Department of Biochemistry, School of Life Sciences, Central University of Rajasthan, NH-8, Bandarsindri, Kishangarh, Ajmer, Rajasthan, 305817, India.
Molecular Modelling and Simulation Laboratory, Department of Molecular Biology and Biotechnology, Tezpur University, Tezpur, Assam, 784028, India.
Mol Divers. 2024 Jun;28(3):1093-1107. doi: 10.1007/s11030-023-10636-4. Epub 2023 Apr 20.
According to the Center for Disease Control and Prevention, as of August 23, 94 countries had confirmed 42,954 Monkeypox Virus cases. As specific monkeypox drugs are not yet developed, the treatment depends on repurposed FDA-approved drugs. According to a recent study, the Monkeypox outbreak is caused by a strain with a unique mutation, raising the likelihood that the virus will develop resistance to current drugs by acquiring mutations in the targets of currently used drugs. The probability of multiple mutations in two or more drug targets at a time is always low than mutation in a single drug target. Therefore, we identified 15 triple-targeting FDA-approved drugs that can inhibit three viral targets, including topoisomerase1, p37, and thymidylate kinase, using high throughput virtual screening approach. Further, the molecular dynamics simulation analysis of the top hits such as Naldemedine and Saquinavir with their respective targets reveals the formation of stable conformational changes of the ligand-protein complexes inside the dynamic biological environment. We suggest further research on these triple-targeting molecules to develop an effective therapy for the currently spreading Monkeypox.
根据疾病控制与预防中心的数据,截至 8 月 23 日,94 个国家已确认 42954 例猴痘病毒病例。由于尚未开发出特定的猴痘药物,治疗方法取决于已批准的 FDA 重新利用药物。最近的一项研究表明,猴痘疫情是由一种具有独特突变的菌株引起的,这增加了病毒通过在现有药物靶点获得突变而对现有药物产生抗药性的可能性。同时在两个或多个药物靶点上发生多次突变的概率总是低于单个药物靶点的突变。因此,我们使用高通量虚拟筛选方法,确定了 15 种可抑制三种病毒靶点的三重靶向 FDA 批准药物,包括拓扑异构酶 1、p37 和胸苷酸激酶。此外,通过分子动力学模拟分析,发现 Naldemedine 和 Saquinavir 等顶级化合物与各自的靶点结合形成了稳定的构象变化,在动态的生物环境中。我们建议对这些三重靶向分子进行进一步研究,以开发出针对目前正在传播的猴痘的有效疗法。