Overcoming fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles

Continuing efforts to discover novel means of combating fluconazole resistance in Candida albicans have identified an indole derivative that sensitizes strains demonstrating resistance to fluconazole. This tetracycle (3, ML229) does not appear to act through established Hsp90 or calcineurin pathways...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-05, Vol.22 (9), p.3362-3365
Hauptverfasser:	Youngsaye, Willmen, Dockendorff, Chris, Vincent, Benjamin, Hartland, Cathy L., Bittker, Joshua A., Dandapani, Sivaraman, Palmer, Michelle, Whitesell, Luke, Lindquist, Susan, Schreiber, Stuart L., Munoz, Benito
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal Antifungal agents Biological and medical sciences Candida albicans Candida albicans - drug effects chemistry Chemosensitizer Drug Resistance, Fungal - drug effects Fluconazole Fluconazole - pharmacology General pharmacology indoles Indoles - chemistry Indoles - pharmacology Medical sciences Miscellaneous Molecular libraries probe production center network (MLPCN) Pharmacology. Drug treatments Saccharomyces cerevisiae Signal Transduction
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Beschreibung
Zusammenfassung:	Continuing efforts to discover novel means of combating fluconazole resistance in Candida albicans have identified an indole derivative that sensitizes strains demonstrating resistance to fluconazole. This tetracycle (3, ML229) does not appear to act through established Hsp90 or calcineurin pathways to chemosensitize C. albicans, as determined in Saccharomyces cerevisiae models, and may be a useful probe to uncover alternative resistance pathways.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.02.035