Fungal sphingolipids: role in the regulation of virulence and potential as targets for future antifungal therapies

Expert Rev Anti Infect Ther. 2020 Nov;18(11):1083-1092. doi: 10.1080/14787210.2020.1792288. Epub 2020 Jul 16.

Abstract

Introduction: The antifungal therapy currently available includes three major classes of drugs: polyenes, azoles and echinocandins. However, the clinical use of these compounds faces several challenges: while polyenes are toxic to the host, antifungal resistance to azoles and echinocandins has been reported.

Areas covered: Fungal sphingolipids (SL) play a pivotal role in growth, morphogenesis and virulence. In addition, fungi possess unique enzymes involved in SL synthesis, leading to the production of lipids which are absent or differ structurally from the mammalian counterparts. In this review, we address the enzymatic reactions involved in the SL synthesis and their relevance to the fungal pathogenesis, highlighting their potential as targets for novel drugs and the inhibitors described so far.

Expert opinion: The pharmacological inhibition of fungal serine palmitoyltransferase depends on the development of specific drugs, as myriocin also targets the mammalian enzyme. Inhibitors of ceramide synthase might constitute potent antifungals, by depleting the pool of complex SL and leading to the accumulation of the toxic intermediates. Acylhydrazones and aureobasidin A, which inhibit GlcCer and IPC synthesis, are not toxic to the host and effectively treat invasive mycoses, emerging as promising new classes of antifungal drugs.

Keywords: Fungi; antifungal therapy; glucosylceramide; inositol phosphorylceramide; sphingolipids.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacology*
  • Drug Development
  • Drug Resistance, Fungal
  • Fungi / drug effects
  • Fungi / pathogenicity
  • Humans
  • Mycoses / drug therapy*
  • Mycoses / microbiology
  • Sphingolipids / metabolism*
  • Virulence

Substances

  • Antifungal Agents
  • Sphingolipids