• 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
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  • 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>
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