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Medientyp:
E-Artikel
Titel:
Sensitive Assay for Antifungal Activity of Glucan Synthase Inhibitors That Uses Germ Tube Formation in Candida albicans as an End Point
Beteiligte:
Brayman, Timothy G.;
Wilks, John W.
Erschienen:
American Society for Microbiology, 2003
Erschienen in:Antimicrobial Agents and Chemotherapy
Sprache:
Englisch
DOI:
10.1128/aac.47.10.3305-3310.2003
ISSN:
0066-4804;
1098-6596
Entstehung:
Anmerkungen:
Beschreibung:
<jats:title>ABSTRACT</jats:title>
<jats:p>
We implemented a simple, sensitive, objective, and rapid cellular assay to reveal the antifungal activity of a novel class of glucan synthase inhibitors. The assay, especially useful for early drug discovery, measures the transformation of
<jats:italic>Candida albicans</jats:italic>
from the yeast form to the hyphal form. Test compounds were ranked by potency (50% inhibitory concentration) and efficacy (percent inhibition of germ tube formation); the intra-assay coefficients of variation for these parameters were 17 and 5%, respectively. The germ tube formation assay proved useful for the early-stage antifungal characterization of a novel class of glucan synthase inhibitors discovered at Pharmacia. Drug concentrations required in this assay to inhibit germ tube formation were lower for 90% of the novel compounds than the concentrations required to determine MICs. The method may have utility for other mechanistic classes of antifungal compounds during the hit-to-lead transition of drug discovery.
</jats:p>