Literature DB >> 19253321

Cerulenin analogues as inhibitors of efflux pumps in drug-resistant Candida albicans.

Florian Diwischek1, Joachim Morschhäuser, Ulrike Holzgrabe.   

Abstract

Overexpression of the ABC transporters Cdr1 and Cdr2 or the major facilitator Mdr1 causes multidrug resistance in the human fungal pathogen Candida albicans. The fatty acid synthesis inhibitor cerulenin and the structurally unrelated Golgi transport inhibitor brefeldin A are substrates for both types of efflux pumps in Candida albicans. In an effort to overcome efflux pump-mediated drug resistance in Candida albicans, cerulenin analogues were generated using a variety of synthesis pathways. The so obtained cerulenin derivatives were tested on multidrug-resistant Candida albicans isolates which constitutively overexpress either Mdr1 or Cdr1 and Cdr2. Some of these compounds were found to decrease Mdr1-mediated resistance to brefeldin A up to eightfold compared to the control.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19253321     DOI： 10.1002/ardp.200800160

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN： 0365-6233            Impact factor:   3.751


  6 in total

Review 1.  Xenobiotic efflux in bacteria and fungi: a genomics update.

Authors:  Ravi D Barabote; Jose Thekkiniath; Richard E Strauss; Govindsamy Vediyappan; Joe A Fralick; Michael J San Francisco
Journal:  Adv Enzymol Relat Areas Mol Biol       Date:  2011

Review 2.  Targeting efflux pumps to overcome antifungal drug resistance.

Authors:  Ann R Holmes; Tony S Cardno; J Jacob Strouse; Irena Ivnitski-Steele; Mikhail V Keniya; Kurt Lackovic; Brian C Monk; Larry A Sklar; Richard D Cannon
Journal:  Future Med Chem       Date:  2016-07-27       Impact factor: 3.808

3.  Synthetic Organotellurium Compounds Sensitize Drug-Resistant Candida albicans Clinical Isolates to Fluconazole.

Authors:  L F Reis de Sá; F T Toledo; A C Gonçalves; B A Sousa; A A Dos Santos; P F Brasil; V A Duarte da Silva; A C Tessis; J A Ramos; M A Carvalho; E Lamping; A Ferreira-Pereira
Journal:  Antimicrob Agents Chemother       Date:  2016-12-27       Impact factor: 5.191

4.  The monoamine oxidase A inhibitor clorgyline is a broad-spectrum inhibitor of fungal ABC and MFS transporter efflux pump activities which reverses the azole resistance of Candida albicans and Candida glabrata clinical isolates.

Authors:  Ann R Holmes; Mikhail V Keniya; Irena Ivnitski-Steele; Brian C Monk; Erwin Lamping; Larry A Sklar; Richard D Cannon
Journal:  Antimicrob Agents Chemother       Date:  2011-12-27       Impact factor: 5.191

5.  Inhibitors of the Candida albicans Major Facilitator Superfamily Transporter Mdr1p Responsible for Fluconazole Resistance.

Authors:  Mikhail V Keniya; Edmond Fleischer; Anette Klinger; Richard D Cannon; Brian C Monk
Journal:  PLoS One       Date:  2015-05-07       Impact factor: 3.240

6.  Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives.

Authors:  Izabela Ła̧cka; Marek T Konieczny; Anita Bułakowska; Marie Kodedová; Dana Gašková; Indresh K Maurya; Rajendra Prasad; Sławomir Milewski
Journal:  Front Microbiol       Date:  2015-08-05       Impact factor: 5.640
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.