Scientific Publications

Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates.

Publication TypeJournal Article
AuthorsYoungsaye, W., Vincent B., Hartland CL, Morgan BJ, Buhrlage SJ, Johnston S., Bittker JA, Macpherson L., Dandapani S., Palmer M., Whitesell L., Lindquist S., Schreiber SL, and Munoz B.
AbstractThe effectiveness of the potent antifungal drug fluconazole is being compromised by the rise of drug-resistant fungal pathogens. While inhibition of Hsp90 or calcineurin can reverse drug resistance in Candida, such inhibitors also impair the homologous human host protein and fungal-selective chemosensitizers remain rare. The MLPCN library was screened to identify compounds that selectively reverse fluconazole resistance in a Candida albicans clinical isolate, while having no antifungal activity when administered as a single agent. A piperazinyl quinoline was identified as a new small-molecule probe (ML189) satisfying these criteria.
Year of Publication2011
JournalBioorganic & medicinal chemistry letters
Date Published (YYYY/MM/DD)2011/09/15
ISSN Number0960-894X