Abstract
We have transformed Saccharomyces cerevisiae with a genomic library contained in the replicative vector pFL44. The resulting transformants were screened for resistance to fenpropidin, a specific inhibitor of sterol 14-reductase. A plasmid was isolated that transformed yeast both to resistance to fenpropidin and to an increased specific activity of sterol 14-reductase. Sterol analysis of transformed cells grown in the presence of increasing concentrations of the inhibitor confirmed that resistance was a consequence of over-production of sterol 14-reductase. By chromosomal gene disruption, we have, for the first time, constructed yeast strains defective in sterol 14-reductase. As expected, since yeast in unable to take up sterols in aerobiosis, the disrupted strains do not grow in the presence of oxygen, even if exogenous sterols are supplied. However, disrupted cells grow in anaerobiosis with exogenous oleic acid and ergosterol supplements. They also grow in aerobiosis if they bear an additional mutation allowing sterol uptake. In this last growth condition the cells require a "sparking" ergosterol supplementation (25 nM) and accumulate ignosterol (ergosta-8,14-dienol) as the end-product of the sterol pathway. These results reveal that ignosterol is not obviously toxic to yeast membranes and strongly suggest that the molecular basis of the antifungal-activity morpholine and piperidine is directly related to the specific inhibition of ergosterol formation.
MeSH Terms
Cloning, Molecular/methods
Drug Resistance, Microbial
Ergosterol/analogs & derivatives,biosynthesis,metabolism
Genes, Fungal
Mutagenesis, Site-Directed
Oxidoreductases/antagonists & inhibitors,genetics
Piperidines/pharmacology
Saccharomyces cerevisiae/enzymology,genetics,growth & development
Transformation, Genetic
Chemicals
Piperidines
fenpropidine
Oxidoreductases
delta(14)-sterol reductase
ignosterol
Ergosterol
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Marcireau C
Laboratoire de Biochimie et Génétique des Microorganismes, Université de Poitiers, France.
Guyonnet D
Karst F
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