Disulfide Bond Engineering of Soluble ACE2 for Thermal Stability Enhancement

Int J Mol Sci. 2024 Sep 14;25(18):9919. doi: 10.3390/ijms25189919.

Abstract

Although the primary pandemic of SARS-CoV-2 is over, there are concerns about the resurgence of the next wave of related viruses, including a wide range of variant viruses. The soluble ACE2 (sACE2) inhibits the SARS-CoV-2 spike protein ACE2 interaction and has potential as a variant-independent therapeutic against SARS-CoV-2. Here, we introduce novel disulfide bonds in the wild-type sACE2-Fc by structure-guided mutagenesis, aiming to improve its stability. The stability of each mutant was assessed by a thermal shift assay to screen mutants with increased thermal stability. As a result, we identified a mutant sACE2-Fc with a significantly increased melting temperature. X-ray crystal structure determination of the sACE2 mutant confirmed the correct formation of the designed disulfide bond, and there were no significant structural disturbances. We also proved that the thermostable sACE2-Fc preserved the spike protein binding affinity comparable to the wild-type sACE2-Fc in both molecular and cellular environments, suggesting its therapeutic potential.

Keywords: SARS-CoV-2; disulfide bond; soluble ACE2; thermal stability enhancement; variant-independent therapeutics.

MeSH terms

  • Angiotensin-Converting Enzyme 2* / chemistry
  • Angiotensin-Converting Enzyme 2* / genetics
  • Angiotensin-Converting Enzyme 2* / metabolism
  • COVID-19 / virology
  • Crystallography, X-Ray
  • Disulfides* / chemistry
  • Disulfides* / metabolism
  • Humans
  • Mutation
  • Protein Binding
  • Protein Engineering / methods
  • Protein Stability*
  • SARS-CoV-2* / genetics
  • SARS-CoV-2* / metabolism
  • Spike Glycoprotein, Coronavirus* / chemistry
  • Spike Glycoprotein, Coronavirus* / genetics
  • Spike Glycoprotein, Coronavirus* / metabolism

Substances

  • Angiotensin-Converting Enzyme 2
  • Disulfides
  • Spike Glycoprotein, Coronavirus
  • ACE2 protein, human
  • spike protein, SARS-CoV-2

Grants and funding

This research was funded by the National Research Foundation, Korea (grant number 2021M3A9G8024747).