Site-directed M2 proton channel inhibitors enable synergistic combination therapy for rimantadine-resistant pandemic influenza

PLoS Pathog. 2020 Aug 11;16(8):e1008716. doi: 10.1371/journal.ppat.1008716. eCollection 2020 Aug.

Abstract

Pandemic influenza A virus (IAV) remains a significant threat to global health. Preparedness relies primarily upon a single class of neuraminidase (NA) targeted antivirals, against which resistance is steadily growing. The M2 proton channel is an alternative clinically proven antiviral target, yet a near-ubiquitous S31N polymorphism in M2 evokes resistance to licensed adamantane drugs. Hence, inhibitors capable of targeting N31 containing M2 (M2-N31) are highly desirable. Rational in silico design and in vitro screens delineated compounds favouring either lumenal or peripheral M2 binding, yielding effective M2-N31 inhibitors in both cases. Hits included adamantanes as well as novel compounds, with some showing low micromolar potency versus pandemic "swine" H1N1 influenza (Eng195) in culture. Interestingly, a published adamantane-based M2-N31 inhibitor rapidly selected a resistant V27A polymorphism (M2-A27/N31), whereas this was not the case for non-adamantane compounds. Nevertheless, combinations of adamantanes and novel compounds achieved synergistic antiviral effects, and the latter synergised with the neuraminidase inhibitor (NAi), Zanamivir. Thus, site-directed drug combinations show potential to rejuvenate M2 as an antiviral target whilst reducing the risk of drug resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / pharmacology
  • Drug Resistance, Viral
  • Drug Synergism
  • Drug Therapy, Combination
  • Humans
  • Influenza A Virus, H1N1 Subtype / drug effects*
  • Influenza A Virus, H1N1 Subtype / genetics
  • Influenza A Virus, H1N1 Subtype / metabolism
  • Influenza, Human / drug therapy
  • Influenza, Human / virology*
  • Rimantadine / pharmacology*
  • Viral Matrix Proteins / antagonists & inhibitors*
  • Viral Matrix Proteins / genetics
  • Viral Matrix Proteins / metabolism
  • Zanamivir / pharmacology*

Substances

  • Antiviral Agents
  • M2 protein, Influenza A virus
  • Viral Matrix Proteins
  • Rimantadine
  • Zanamivir