Document Detail

Inhibitory effects of gallic acid ester derivatives on Saccharomyces cerevisiae multidrug resistance protein Pdr5p.
MedLine Citation:
PMID:  20132313     Owner:  NLM     Status:  MEDLINE    
Overexpression of the Saccharomyces cerevisiae ABC transporter Pdr5p confers resistance to a range of structurally unrelated xenobiotics. This property allows Pdr5p to be used as a target for novel multidrug resistance reversal reagents or chemosensitizers. Herein, we report the effects of gallic acid derivatives with substitutions either on the ester moiety or in the benzene ring on the activity of Pdr5p. Compounds with a longer side chain (8-16 carbons) resulted in greater inhibition of Pdr5p ATPase. Derivatives with side chains of 8-12 carbons that retained hydroxyl groups on the benzene ring extensively inhibited Pdr5p ATPase activity. These compounds almost completely inhibited the efflux of the Pdr5p fluorescent substrate Rhodamine 6G and at 25 muM chemosensitized the Pdr5p-overexpressing strain AD124567 to fluconazole (0.4 mg mL(-1)). Gallic acid derivatives may be a new class of Pdr5p inhibitors.
Luciana Pereira Rangel; Márcio Fritzen; Rosendo Augusto Yunes; Paulo César Leal; Tânia Beatriz Creczynski-Pasa; Antônio Ferreira-Pereira
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-02-01
Journal Detail:
Title:  FEMS yeast research     Volume:  10     ISSN:  1567-1364     ISO Abbreviation:  FEMS Yeast Res.     Publication Date:  2010 May 
Date Detail:
Created Date:  2010-06-04     Completed Date:  2010-09-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101085384     Medline TA:  FEMS Yeast Res     Country:  England    
Other Details:
Languages:  eng     Pagination:  244-51     Citation Subset:  IM    
Laboratório de Bioquímica Microbiana, Departamento de Microbiologia Geral/IMPPG, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil.
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MeSH Terms
ATP-Binding Cassette Transporters / antagonists & inhibitors*
Adenosine Triphosphatases / antagonists & inhibitors
Antifungal Agents / metabolism*
Drug Resistance, Multiple, Fungal / drug effects*
Enzyme Inhibitors / pharmacology*
Gallic Acid / analogs & derivatives*,  chemistry,  pharmacology*
Molecular Structure
Rhodamines / metabolism
Saccharomyces cerevisiae / drug effects*,  growth & development
Saccharomyces cerevisiae Proteins / antagonists & inhibitors*
Structure-Activity Relationship
Reg. No./Substance:
0/ATP-Binding Cassette Transporters; 0/Antifungal Agents; 0/Enzyme Inhibitors; 0/PDR5 protein, S cerevisiae; 0/Rhodamines; 0/Saccharomyces cerevisiae Proteins; 149-91-7/Gallic Acid; 989-38-8/rhodamine 6G; EC 3.6.1.-/Adenosine Triphosphatases

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