Characterization of Critical Determinants of ACE2-SARS CoV-2 RBD Interaction

Int J Mol Sci. 2021 Feb 25;22(5):2268. doi: 10.3390/ijms22052268.

Abstract

Despite sequence similarity to SARS-CoV-1, SARS-CoV-2 has demonstrated greater widespread virulence and unique challenges to researchers aiming to study its pathogenicity in humans. The interaction of the viral receptor binding domain (RBD) with its main host cell receptor, angiotensin-converting enzyme 2 (ACE2), has emerged as a critical focal point for the development of anti-viral therapeutics and vaccines. In this study, we selectively identify and characterize the impact of mutating certain amino acid residues in the RBD of SARS-CoV-2 and in ACE2, by utilizing our recently developed NanoBiT technology-based biosensor as well as pseudotyped-virus infectivity assays. Specifically, we examine the mutational effects on RBD-ACE2 binding ability, efficacy of competitive inhibitors, as well as neutralizing antibody activity. We also look at the implications the mutations may have on virus transmissibility, host susceptibility, and the virus transmission path to humans. These critical determinants of virus-host interactions may provide more effective targets for ongoing vaccines, drug development, and potentially pave the way for determining the genetic variation underlying disease severity.

Keywords: NanoLuc Binary Technology; SARS-CoV-2; angiotensin-converting enzyme 2; bioluminescence; drug development; receptor binding domain; spike protein; vaccine development.

MeSH terms

  • Amino Acid Sequence
  • Angiotensin-Converting Enzyme 2 / chemistry*
  • Angiotensin-Converting Enzyme 2 / genetics
  • Angiotensin-Converting Enzyme 2 / metabolism*
  • Antibodies, Neutralizing / immunology
  • Antiviral Agents / pharmacology
  • Binding Sites
  • COVID-19 / immunology
  • COVID-19 / metabolism*
  • COVID-19 / virology*
  • COVID-19 Drug Treatment
  • HEK293 Cells
  • Host Microbial Interactions
  • Humans
  • Models, Molecular
  • Mutation
  • Protein Binding
  • Protein Interaction Domains and Motifs
  • Receptors, Virus / chemistry
  • Receptors, Virus / metabolism
  • SARS-CoV-2 / drug effects
  • SARS-CoV-2 / metabolism*
  • Sequence Alignment
  • Spike Glycoprotein, Coronavirus / chemistry*
  • Spike Glycoprotein, Coronavirus / metabolism*

Substances

  • Antibodies, Neutralizing
  • Antiviral Agents
  • Receptors, Virus
  • Spike Glycoprotein, Coronavirus
  • ACE2 protein, human
  • Angiotensin-Converting Enzyme 2