Ghorbani Mahdi, Brooks Bernard R, Klauda Jeffery B
bioRxiv. 2020 Jun 27:2020.06.27.175448. doi: 10.1101/2020.06.27.175448.
The novel coronavirus (nCOV-2019) outbreak has put the world on edge, causing millions of cases and hundreds of thousands of deaths all around the world, as of June 2020, let alone the societal and economic impacts of the crisis. The spike protein of nCOV-2019 resides on the virion's surface mediating coronavirus entry into host cells by binding its receptor binding domain (RBD) to the host cell surface receptor protein, angiotensin converter enzyme (ACE2). Our goal is to provide a detailed structural mechanism of how nCOV-2019 recognizes and establishes contacts with ACE2 and its difference with an earlier coronavirus SARS-COV in 2002 via extensive molecular dynamics (MD) simulations. Numerous mutations have been identified in the RBD of nCOV-2019 strains isolated from humans in different parts of the world. In this study, we investigated the effect of these mutations as well as other Ala-scanning mutations on the stability of RBD/ACE2 complex. It is found that most of the naturally-occurring mutations to the RBD either strengthen or have the same binding affinity to ACE2 as the wild-type nCOV-2019. This may have implications for high human-to-human transmission of coronavirus in regions where these mutations have been found as well as any vaccine design endeavors since these mutations could act as antibody escape mutants. Furthermore, in-silico Ala-scanning and long-timescale MD simulations, highlight the crucial role of the residues at the interface of RBD and ACE2 that may be used as potential pharmacophores for any drug development endeavors. From an evolutional perspective, this study also identifies how the virus has evolved from its predecessor SARS-COV and how it could further evolve to become more infectious.
新型冠状病毒(nCOV - 2019)的爆发让全球陷入紧张状态,截至2020年6月,已在全球造成数百万感染病例和数十万死亡病例,更不用说这场危机对社会和经济的影响了。nCOV - 2019的刺突蛋白位于病毒粒子表面,通过将其受体结合域(RBD)与宿主细胞表面受体蛋白血管紧张素转换酶(ACE2)结合,介导冠状病毒进入宿主细胞。我们的目标是通过广泛的分子动力学(MD)模拟,详细阐述nCOV - 2019如何识别并与ACE2建立联系,以及它与2002年的早期冠状病毒SARS - COV的差异。在从世界不同地区分离出的nCOV - 2019毒株的RBD中,已发现了许多突变。在本研究中,我们调查了这些突变以及其他丙氨酸扫描突变对RBD/ACE2复合物稳定性的影响。研究发现,RBD的大多数自然发生的突变要么增强了与ACE2的结合亲和力,要么与野生型nCOV - 2019具有相同的结合亲和力。这可能对在发现这些突变的地区冠状病毒的高人际传播以及任何疫苗设计工作都有影响,因为这些突变可能充当抗体逃逸突变体。此外,计算机模拟的丙氨酸扫描和长时间尺度的MD模拟突出了RBD和ACE2界面处残基的关键作用,这些残基可能被用作任何药物开发工作的潜在药效基团。从进化的角度来看,这项研究还确定了该病毒如何从其前身SARS - COV进化而来,以及它如何进一步进化以变得更具传染性。