| Literature DB >> 21802942 |
Willmen Youngsaye1, Benjamin Vincent, Cathy L Hartland, Barbara J Morgan, Sara J Buhrlage, Stephen Johnston, Joshua A Bittker, Lawrence MacPherson, Sivaraman Dandapani, Michelle Palmer, Luke Whitesell, Susan Lindquist, Stuart L Schreiber, Benito Munoz.
Abstract
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.Entities:
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Year: 2011 PMID： 21802942 PMCID： PMC3287054 DOI： 10.1016/j.bmcl.2011.06.105
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823