Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates
Author(s)Youngsaye, Willmen; Vincent, Benjamin; Hartland, Cathy L.; Morgan, Barbara J.; Buhrlage, Sara J.; Johnston, Stephen; Bittker, Joshua A.; MacPherson, Lawrence; Dandapani, Sivaraman; Palmer, Michelle; Whitesell, Luke; Lindquist, Susan; Schreiber, Stuart L.; Munoz, Benito; ... Show more Show less
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The 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.
DepartmentMassachusetts Institute of Technology. Department of Biology
Bioorganic & Medicinal Chemistry Letters
Youngsaye, Willmen, Benjamin Vincent, Cathy L. Hartland, Barbara J. Morgan, Sara J. Buhrlage, Stephen Johnston, Joshua A. Bittker, et al. “Piperazinyl Quinolines as Chemosensitizers to Increase Fluconazole Susceptibility of Candida Albicans Clinical Isolates.” Bioorganic & Medicinal Chemistry Letters 21, no. 18 (September 2011): 5502–5505.
Author's final manuscript