Overview of antiviral drug candidates targeting coronaviral 3C-like main proteases

FEBS J. 2021 Sep;288(17):5089-5121. doi: 10.1111/febs.15696. Epub 2021 Feb 1.

Abstract

Coronaviruses (CoVs) are positive single-stranded RNA viruses that cause severe respiratory syndromes in humans, including severe acute respiratory syndrome (SARS) and Middle East respiratory syndrome (MERS). Coronavirus disease 2019 (COVID-19) caused by a novel severe acute respiratory syndrome CoV (SARS-CoV-2) at the end of 2019 became a global pandemic. The 3C-like cysteine protease (3CLpro) processes viral polyproteins to yield mature non-structural proteins, thus playing an important role in the CoV life cycle, and therefore is considered as a prominent target for antiviral drugs. To date, many 3CLpro inhibitors have been reported, and their molecular mechanisms have been illustrated. Here, we briefly introduce the structural features of 3CLpro of the human-related SARS-CoV, MERS-CoV and SARS-CoV-2, and explore the potency and mechanism of their cognate inhibitors. This information will shed light on the development and optimization of CoV 3CLpro inhibitors, which may benefit the further designation of therapeutic strategies for treating CoV diseases.

Keywords: 3C-like cysteine protease; MERS; SARS; coronaviruses; inhibitor; main protease; structure.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / therapeutic use
  • COVID-19 / enzymology
  • COVID-19 / virology
  • COVID-19 Drug Treatment*
  • Coronavirus 3C Proteases / antagonists & inhibitors
  • Coronavirus 3C Proteases / chemistry
  • Coronavirus 3C Proteases / genetics*
  • Humans
  • Molecular Targeted Therapy
  • Pandemics
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / therapeutic use*
  • SARS-CoV-2 / drug effects*
  • SARS-CoV-2 / enzymology
  • SARS-CoV-2 / pathogenicity
  • Viral Nonstructural Proteins

Substances

  • Antiviral Agents
  • Protease Inhibitors
  • Viral Nonstructural Proteins
  • 3C-like proteinase, SARS-CoV-2
  • Coronavirus 3C Proteases