Candida glabrata erg1 mutant with increased sensitivity to azoles and to low oxygen tension

Antimicrob Agents Chemother. 2004 Jul;48(7):2483-9. doi: 10.1128/AAC.48.7.2483-2489.2004.

Abstract

A Candida glabrata erg1 (Cgerg1) mutant, CgTn201S, was identified by transposon mutagenesis and by increased fluconazole susceptibility. CgERG1 encodes a 489-amino-acid protein which, on the basis of its homology with Saccharomyces cerevisiae ERG1, is a squalene epoxidase essential for ergosterol synthesis. Interruption following codon 475 of CgErg1p decreased the ergosterol content by 50%; caused accumulation of the squalene precursor; increased the levels of susceptibility to fluconazole, itraconazole, and terbinafine; increased the level of resistance to amphotericin B; increased the levels of rhodamine 6G and [(3)H]-fluconazole uptake; reduced the level of growth; and blocked growth under conditions of low oxygen tension. In addition, CgTn201S efficiently took up exogenous cholesterol from cholesterol-containing serum. Cholesterol constituted 34% of the extractable sterols in CgTn201S when it was grown aerobically on serum-containing medium. Under the same conditions, C. albicans contained only 0.1 to 1.2% cholesterol. Exogenous sterols also restored growth under conditions of low oxygen tension. Finally, complementation of the Cgerg1 mutation restored the levels of [(3)H]fluconazole uptake and drug susceptibility to wild-type levels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / metabolism
  • Antifungal Agents / pharmacology*
  • Azoles / metabolism
  • Azoles / pharmacology*
  • Candida glabrata / drug effects*
  • Candida glabrata / genetics*
  • Candida glabrata / metabolism
  • Cholesterol / metabolism
  • Cloning, Molecular
  • DNA Transposable Elements / genetics
  • Drug Resistance, Fungal
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels
  • Fluconazole / metabolism
  • Fluconazole / pharmacology
  • Fluorescent Dyes
  • Genetic Complementation Test
  • Microbial Sensitivity Tests
  • Mutation / genetics*
  • Oxygen / pharmacology*
  • Phenotype
  • Plasmids / genetics
  • Potassium Channels / genetics*
  • Potassium Channels, Voltage-Gated
  • Rhodamines
  • Squalene / metabolism
  • Sterols / metabolism

Substances

  • Antifungal Agents
  • Azoles
  • DNA Transposable Elements
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels
  • Fluorescent Dyes
  • Potassium Channels
  • Potassium Channels, Voltage-Gated
  • Rhodamines
  • Sterols
  • rhodamine 6G
  • Squalene
  • Fluconazole
  • Cholesterol
  • Oxygen