Evidence map›Paper›PMID 25062749›Full record

ArticleBMC microbiology2014

Synthetic organotelluride compounds induce the reversal of Pdr5p mediated fluconazole resistance in Saccharomyces cerevisiae.

Leandro Figueira Reis de Sá, Fabiano Travanca Toledo, Bruno Artur de Sousa, Augusto César Gonçalves, Ana Claudia Tessis, Edison P Wendler, João V Comasseto, Alcindo A Dos Santos, Antonio Ferreira-Pereira

Open access · goldAbstract read
In one paragraph

Article in BMC microbiology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
0.3field-weighted citation impact, top 39% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

11 citing papers in PubMed, 20 citations in OpenAlex.

  1. New Acylglucoses fromPlants (Basel, Switzerland) · 2026
    Article
  2. Antifungal activity of β-lapachone against a fluconazole-resistant Candida auris strain.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2024
    Article
  3. Article
  4. Article
  5. Digoxin Derivatives Sensitize aJournal of fungi (Basel, Switzerland) · 2022
    Article
  6. Review
  7. Article
  8. β-Lapachone enhances the antifungal activity of fluconazole against a Pdr5p-mediated resistant Saccharomyces cerevisiae strain.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2020
    Article
  9. Article
  10. Article
  11. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 5 institutions in 1 country.

Leandro Figueira Reis de Sá
Fabiano Travanca Toledo
Bruno Artur de Sousa
Augusto César Gonçalves
Ana Claudia Tessis
Edison P Wendler
João V Comasseto
Alcindo A Dos SantosInstituto de Microbiologia Paulo de Góes, Departamento de Microbiologia Geral, Laboratório de Bioquímica Microbiana, CCS, Universidade Federal do Rio de Janeiro, Rio de Janeiro/RJ, Brazil. alcindo@iq.usp.br.
Antonio Ferreira-Pereira
Universidade de São Paulo · BRInstituto Butantan · BRUniversidade Federal do Rio de Janeiro · BRRio de Janeiro Federal Institute of Education, Science and Technology · BRUniversidade Federal de São Paulo · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundResistance to fluconazole, a commonly used azole antifungal, is a challenge for the treatment of fungal infections. Resistance can be mediated by overexpression of ABC transporters, which promote drug efflux that requires ATP hydrolysis. The Pdr5p ABC transporter of Saccharomyces cerevisiae is a well-known model used to study this mechanism of antifungal resistance. The present study investigated the effects of 13 synthetic compounds on Pdr5p.

resultsAmong the tested compounds, four contained a tellurium-butane group and shared structural similarities that were absent in the other tested compounds: a lateral hydrocarbon chain and an amide group. These four compounds were capable of inhibiting Pdr5p ATPase activity by more than 90%, they demonstrated IC50 values less than 2 μM and had an uncompetitive pattern of Pdr5p ATPase activity inhibition. These organotellurides did not demonstrate cytotoxicity against human erythrocytes or S. cerevisiae mutant strains (a strain that overexpress Pdr5p and a null mutant strain) even in concentrations above 100 μM. When tested at 100 μM, they could reverse the fluconazole resistance expressed by both the S. cerevisiae mutant strain that overexpress Pdr5p and a clinical isolate of Candida albicans.

conclusionsWe have identified four organotellurides that are promising candidates for the reversal of drug resistance mediated by drug efflux pumps. These molecules will act as scaffolds for the development of more efficient and effective efflux pump inhibitors that can be used in combination therapy with available antifungals.

Indexed as

Antifungal AgentsATP-Binding Cassette TransportersButanesDrug Resistance, FungalEnzyme InhibitorsErythrocytesFluconazoleInhibitory Concentration 50Saccharomyces cerevisiaeSaccharomyces cerevisiae ProteinsTelluriumAntifungal AgentsATP-Binding Cassette TransportersbutaneButanesEnzyme InhibitorsFluconazolePDR5 protein, S cerevisiaeSaccharomyces cerevisiae ProteinsTellurium

Identifiers

PMID25062749
PMCPMC4222501
OpenAlexW2010200283

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.