Dynamic Profiling of β-Coronavirus 3CL Mpro Protease Ligand-Binding Sites

J Chem Inf Model. 2021 Jun 28;61(6):3058-3073. doi: 10.1021/acs.jcim.1c00449. Epub 2021 Jun 14.

Abstract

β-coronavirus (CoVs) alone has been responsible for three major global outbreaks in the 21st century. The current crisis has led to an urgent requirement to develop therapeutics. Even though a number of vaccines are available, alternative strategies targeting essential viral components are required as a backup against the emergence of lethal viral variants. One such target is the main protease (Mpro) that plays an indispensable role in viral replication. The availability of over 270 Mpro X-ray structures in complex with inhibitors provides unique insights into ligand-protein interactions. Herein, we provide a comprehensive comparison of all nonredundant ligand-binding sites available for SARS-CoV2, SARS-CoV, and MERS-CoV Mpro. Extensive adaptive sampling has been used to investigate structural conservation of ligand-binding sites using Markov state models (MSMs) and compare conformational dynamics employing convolutional variational auto-encoder-based deep learning. Our results indicate that not all ligand-binding sites are dynamically conserved despite high sequence and structural conservation across β-CoV homologs. This highlights the complexity in targeting all three Mpro enzymes with a single pan inhibitor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents
  • Binding Sites
  • COVID-19*
  • Humans
  • Ligands
  • Peptide Hydrolases*
  • Protease Inhibitors
  • RNA, Viral
  • SARS-CoV-2

Substances

  • Antiviral Agents
  • Ligands
  • Protease Inhibitors
  • RNA, Viral
  • Peptide Hydrolases