College of Chemistry, Central China Normal University.
College of Chemistry of CCNU.
Brief Bioinform. 2021 Sep 2;22(5). doi: 10.1093/bib/bbaa373.
Protein-nucleic acid interactions play essential roles in many biological processes, such as transcription, replication and translation. In protein-nucleic acid interfaces, hotspot residues contribute the majority of binding affinity toward molecular recognition. Hotspot residues are commonly regarded as potential binding sites for compound molecules in drug design projects. The dynamic property is a considerable factor that affects the binding of ligands. Computational approaches have been developed to expedite the prediction of hotspot residues on protein-nucleic acid interfaces. However, existing approaches overlook hotspot dynamics, despite their essential role in protein function. Here, we report a web server named Hotspots In silico Scanning on Nucleic Acid and Protein Interface (HISNAPI) to analyze hotspot residue dynamics by integrating molecular dynamics simulation and one-step free energy perturbation. HISNAPI is capable of not only predicting the hotspot residues in protein-nucleic acid interfaces but also providing insights into their intensity and correlation of dynamic motion. Protein dynamics have been recognized as a vital factor that has an effect on the interaction specificity and affinity of the binding partners. We applied HISNAPI to the case of SARS-CoV-2 RNA-dependent RNA polymerase, a vital target of the antiviral drug for the treatment of coronavirus disease 2019. We identified the hotspot residues and characterized their dynamic behaviors, which might provide insight into the target site for antiviral drug design. The web server is freely available via a user-friendly web interface at http://chemyang.ccnu.edu.cn/ccb/server/HISNAPI/ and http://agroda.gzu.edu.cn:9999/ccb/server/HISNAPI/.
蛋白质-核酸相互作用在许多生物过程中发挥着重要作用,如转录、复制和翻译。在蛋白质-核酸界面中,热点残基对分子识别贡献了大部分结合亲和力。热点残基通常被认为是药物设计项目中化合物分子的潜在结合位点。动态特性是影响配体结合的一个重要因素。已经开发了计算方法来加速预测蛋白质-核酸界面上的热点残基。然而,现有的方法忽略了热点动力学,尽管它们在蛋白质功能中起着至关重要的作用。在这里,我们报告了一个名为 Hotspots In silico Scanning on Nucleic Acid and Protein Interface (HISNAPI) 的网络服务器,用于通过整合分子动力学模拟和一步自由能微扰来分析核酸和蛋白质界面上的热点残基动力学。HISNAPI 不仅能够预测蛋白质-核酸界面上的热点残基,还能够提供其动态运动强度和相关性的见解。蛋白质动力学已被认为是影响结合伙伴相互作用特异性和亲和力的一个重要因素。我们将 HISNAPI 应用于 SARS-CoV-2 RNA 依赖性 RNA 聚合酶的案例,这是治疗 2019 年冠状病毒病的抗病毒药物的重要靶标。我们确定了热点残基并描述了它们的动态行为,这可能为抗病毒药物设计的靶位提供了一些启示。该网络服务器可通过用户友好的网络界面免费使用,网址为 http://chemyang.ccnu.edu.cn/ccb/server/HISNAPI/ 和 http://agroda.gzu.edu.cn:9999/ccb/server/HISNAPI/。