Calcineurin in fungal virulence and drug resistance: Prospects for harnessing targeted inhibition of calcineurin for an antifungal therapeutic approach

Virulence. 2017 Feb 17;8(2):186-197. doi: 10.1080/21505594.2016.1201250. Epub 2016 Jun 20.

Abstract

Increases in the incidence and mortality due to the major invasive fungal infections such as aspergillosis, candidiasis and cryptococcosis caused by the species of Aspergillus, Candida and Cryptococcus, are a growing threat to the immunosuppressed patient population. In addition to the limited armamentarium of the current classes of antifungal agents available (pyrimidine analogs, polyenes, azoles, and echinocandins), their toxicity, efficacy and the emergence of resistance are major bottlenecks limiting successful patient outcomes. Although these drugs target distinct fungal pathways, there is an urgent need to develop new antifungals that are more efficacious, fungal-specific, with reduced or no toxicity and simultaneously do not induce resistance. Here we review several lines of evidence which indicate that the calcineurin signaling pathway, a target of the immunosuppressive drugs FK506 and cyclosporine A, orchestrates growth, virulence and drug resistance in a variety of fungal pathogens and can be exploited for novel antifungal drug development.

Keywords: FK506; FKBP12; Hsp90; antifungals; azoles; calcineurin; cyclosporine A; drug resistance; echinocandins; virulence.

Publication types

  • Review

MeSH terms

  • Antifungal Agents / pharmacology
  • Antifungal Agents / therapeutic use*
  • Aspergillosis / drug therapy
  • Calcineurin / metabolism*
  • Calcineurin Inhibitors / pharmacology
  • Calcineurin Inhibitors / therapeutic use*
  • Candida albicans / drug effects
  • Candidiasis / drug therapy
  • Cyclosporine / therapeutic use
  • Drug Discovery / methods*
  • Drug Resistance, Fungal*
  • Echinocandins / therapeutic use
  • Fungi / drug effects
  • Fungi / metabolism
  • Fungi / pathogenicity*
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors
  • HSP90 Heat-Shock Proteins / metabolism
  • Humans
  • Microbial Sensitivity Tests
  • Signal Transduction / drug effects
  • Tacrolimus / therapeutic use
  • Tacrolimus Binding Protein 1A / metabolism
  • Virulence

Substances

  • Antifungal Agents
  • Calcineurin Inhibitors
  • Echinocandins
  • HSP90 Heat-Shock Proteins
  • Cyclosporine
  • Calcineurin
  • Tacrolimus Binding Protein 1A
  • Tacrolimus