A trimeric human angiotensin-converting enzyme 2 as an anti-SARS-CoV-2 agent

Nat Struct Mol Biol. 2021 Feb;28(2):202-209. doi: 10.1038/s41594-020-00549-3. Epub 2021 Jan 11.

Abstract

Effective intervention strategies are urgently needed to control the COVID-19 pandemic. Human angiotensin-converting enzyme 2 (ACE2) is a membrane-bound carboxypeptidase that forms a dimer and serves as the cellular receptor for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). ACE2 is also a key negative regulator of the renin-angiotensin system that modulates vascular functions. We report here the properties of a trimeric ACE2 ectodomain variant, engineered using a structure-based approach. The trimeric ACE2 variant has a binding affinity of ~60 pM for the spike protein of SARS‑CoV‑2 (compared with 77 nM for monomeric ACE2 and 12-22 nM for dimeric ACE2 constructs), and its peptidase activity and the ability to block activation of angiotensin II receptor type 1 in the renin-angiotensin system are preserved. Moreover, the engineered ACE2 potently inhibits SARS‑CoV‑2 infection in cell culture. These results suggest that engineered, trimeric ACE2 may be a promising anti-SARS-CoV-2 agent for treating COVID-19.

MeSH terms

  • Angiotensin-Converting Enzyme 2 / chemistry*
  • Angiotensin-Converting Enzyme 2 / genetics
  • Angiotensin-Converting Enzyme 2 / therapeutic use
  • Antiviral Agents / chemistry*
  • Antiviral Agents / therapeutic use
  • COVID-19 Drug Treatment*
  • Cryoelectron Microscopy
  • Humans
  • Models, Molecular
  • Protein Engineering
  • Protein Multimerization
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / genetics
  • Recombinant Proteins / therapeutic use
  • SARS-CoV-2 / physiology

Substances

  • Antiviral Agents
  • Recombinant Proteins
  • ACE2 protein, human
  • Angiotensin-Converting Enzyme 2