Alpha-1 antitrypsin inhibits TMPRSS2 protease activity and SARS-CoV-2 infection

Nat Commun. 2021 Mar 19;12(1):1726. doi: 10.1038/s41467-021-21972-0.

Abstract

SARS-CoV-2 is a respiratory pathogen and primarily infects the airway epithelium. As our knowledge about innate immune factors of the respiratory tract against SARS-CoV-2 is limited, we generated and screened a peptide/protein library derived from bronchoalveolar lavage for inhibitors of SARS-CoV-2 spike-driven entry. Analysis of antiviral fractions revealed the presence of α1-antitrypsin (α1AT), a highly abundant circulating serine protease inhibitor. Here, we report that α1AT inhibits SARS-CoV-2 entry at physiological concentrations and suppresses viral replication in cell lines and primary cells including human airway epithelial cultures. We further demonstrate that α1AT binds and inactivates the serine protease TMPRSS2, which enzymatically primes the SARS-CoV-2 spike protein for membrane fusion. Thus, the acute phase protein α1AT is an inhibitor of TMPRSS2 and SARS-CoV-2 entry, and may play an important role in the innate immune defense against the novel coronavirus. Our findings suggest that repurposing of α1AT-containing drugs has prospects for the therapy of COVID-19.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Viral / blood
  • Antiviral Agents / pharmacology
  • COVID-19 / blood
  • COVID-19 Drug Treatment*
  • Caco-2 Cells
  • Humans
  • Immunoglobulin G / blood
  • Molecular Docking Simulation
  • SARS-CoV-2 / drug effects*
  • Serine Endopeptidases / metabolism*
  • Serine Proteinase Inhibitors / pharmacology*
  • Spike Glycoprotein, Coronavirus / metabolism
  • Virus Internalization / drug effects
  • Virus Replication / drug effects
  • alpha 1-Antitrypsin / pharmacology*

Substances

  • Antibodies, Viral
  • Antiviral Agents
  • Immunoglobulin G
  • Serine Proteinase Inhibitors
  • Spike Glycoprotein, Coronavirus
  • alpha 1-Antitrypsin
  • spike protein, SARS-CoV-2
  • Serine Endopeptidases
  • TMPRSS2 protein, human