Abstract

The ongoing pandemic of coronavirus 2 represents a major challenge for global public health authorities. Coronavirus disease 2019 can be fatal especially in elderly people and those with comorbidities. Currently, several vaccines against coronavirus 2 are under application in multiple countries with emergency use authorization. In the same time, many vaccine candidates are under development and assessment. It is worth noting that the design of some of these vaccines depends on the expression of receptor binding domain for viral spike protein to induce host immunity. As such, blocking the spike protein interface with antibodies, peptides or small molecular compounds can impede the ability of coronavirus 2 to invade host cells by intervention with interactions between viral spike protein and cellular angiotensin converting enzyme 2. In this virtual screening study, we have used predictive webservers, molecular docking and dynamics simulation to evaluate the ability of 3000 compounds to interact with interface residues of spike protein receptor binding domain. This library of chemicals was focused by Life Chemicals as potential protein-protein interactions inhibitor. Here, we report that hit compound 7, with IUPAC name of 3‐cyclohexyl‐N‐(4‐{[(1R,9R) ‐6‐oxo‐7,11‐ diazatricyclo [7.3.1.02,7] trideca‐2,4‐dien‐11‐yl] sulfonyl} phenyl) propenamide, may have the capacity to interact with interface of receptor binding domain for viral spike protein and thereby reduce cellular entry of the virus. However, in vitro and in vivo assessments may be required to validate these virtual findings.

Highlights

  • The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative pathogen responsible for the ongoing pandemic of coronavirus disease 2019 (COVID-19) [1]

  • It is worth noting that the design of some of these vaccines depends on the expression of receptor binding domain for viral spike protein to induce host immunity

  • According to World health organization (WHO), as of 18 February 2021, seven anti-COVID-19 vaccines are under emergency use authorization in multiple countries and more than 60 vaccine candidates are under clinical development [10]

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Summary

Introduction

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative pathogen responsible for the ongoing pandemic of coronavirus disease 2019 (COVID-19) [1]. Different platforms have been utilized to produce these COVID-19 vaccines like inactivated virus, protein subunit, recombinant viral-vector and nucleic acid (DNA and mRNA) Some of these vaccines have focused on the expression of fulllength SARS-CoV-2 spike protein inside human body to elicit immune response, other vaccines used only the receptor binding domain (RBD) of spike protein to induce immunity [11]. The sequence of amino acids for RBD of SARS-CoV-2 spike glycoprotein is presented in Fig. 1 (C), RBD residues involved in interaction with ACE2 are surrounded by orange line. In this virtual screening study, we have used a proteinprotein interactions (PPIs) focused library of compounds from Life Chemicals database. According to rule of four, a compound may have the potential to inhibit protein-protein interactions (PPIs) if it possesses the following four chemical criteria: a molecular weight (M.W.) ≥ 400 g/ mol, a calculated logarithm of partition coefficient (cLog P) ≥ 4, the number of rings ≥ 4 and the number of hydrogen bond acceptor (HBA) ≥ 4 [14,15]

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