Department of Chemistry, University of Vermont, Burlington, VT, 05405, USA.
Sci Rep. 2021 Aug 11;11(1):16307. doi: 10.1038/s41598-021-95826-6.
Structure-based drug design targeting the SARS-CoV-2 virus has been greatly facilitated by available virus-related protein structures. However, there is an urgent need for effective, safe small-molecule drugs to control the spread of the virus and variants. While many efforts are devoted to searching for compounds that selectively target individual proteins, we investigated the potential interactions between eight proteins related to SARS-CoV-2 and more than 600 compounds from a traditional Chinese medicine which has proven effective at treating the viral infection. Our original ensemble docking and cooperative docking approaches, followed by a total of over 16-micorsecond molecular simulations, have identified at least 9 compounds that may generally bind to key SARS-CoV-2 proteins. Further, we found evidence that some of these compounds can simultaneously bind to the same target, potentially leading to cooperative inhibition to SARS-CoV-2 proteins like the Spike protein and the RNA-dependent RNA polymerase. These results not only present a useful computational methodology to systematically assess the anti-viral potential of small molecules, but also point out a new avenue to seek cooperative compounds toward cocktail therapeutics to target more SARS-CoV-2-related proteins.
基于结构的药物设计针对 SARS-CoV-2 病毒,得益于现有与病毒相关的蛋白质结构,取得了很大的进展。然而,迫切需要有效的、安全的小分子药物来控制病毒和变体的传播。虽然许多努力都致力于寻找选择性针对单个蛋白质的化合物,但我们研究了与 SARS-CoV-2 相关的 8 种蛋白质与超过 600 种来自中药的化合物之间的潜在相互作用,这些化合物已被证明可有效治疗病毒感染。我们最初的整体对接和协同对接方法,加上总共超过 16 微秒的分子模拟,已经确定了至少 9 种可能普遍与关键 SARS-CoV-2 蛋白结合的化合物。此外,我们发现了一些证据表明,这些化合物中的一些可以同时与同一目标结合,从而可能导致对 SARS-CoV-2 蛋白(如 Spike 蛋白和 RNA 依赖性 RNA 聚合酶)的协同抑制。这些结果不仅提出了一种有用的计算方法来系统评估小分子的抗病毒潜力,而且还指出了一条新的途径来寻找针对鸡尾酒疗法的协同化合物,以针对更多与 SARS-CoV-2 相关的蛋白质。