Literature DB >> 35041505

Palmarumycin P3 Reverses Mrr1-Mediated Azole Resistance by Blocking the Efflux Pump Mdr1.

Minghui Song1, Ming Zhang2, Jinghui Lu1, Fei Xie3, Jintong Song1, Xiaoyi Luan1, Xuben Hou4, Hongxiang Lou1, Wenqiang Chang1.   

Abstract

Palmarumycin P3 (PP3) reduces fluconazole-induced MDR1 transcription to reverse azole resistance in clinical Candida strains. Here, we demonstrated that PP3 restores the susceptibility to several antifungal drugs for Candida albicans strains with gain-of-function mutations in the transcription factor Mrr1. In addition, PP3 inhibits the efflux of Mdr1 substrates by C. albicans strains harboring hyperactive MRR1 alleles. Molecular docking revealed that PP3 is a potential Mdr1 blocker that binds to the substrate binding pocket of Mdr1.

Entities:  

Keywords:  Candida albicans; Mdr1; Mrr1; azole resistance; palmarumycin P3

Mesh：

Substances：

Year:  2022        PMID： 35041505      PMCID： PMC8923160          DOI： 10.1128/aac.02126-21

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.938


  18 in total

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Journal:  J Comput Chem       Date:  2010-01-30       Impact factor: 3.376

Review 4.  Resistance to antifungal therapies.

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Journal:  Essays Biochem       Date:  2017-03-03       Impact factor: 8.000

5.  Overexpression of the MDR1 gene is sufficient to confer increased resistance to toxic compounds in Candida albicans.

Authors:  Davina Hiller; Dominique Sanglard; Joachim Morschhäuser
Journal:  Antimicrob Agents Chemother       Date:  2006-04       Impact factor: 5.191

6.  Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates.

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Journal:  Cell       Date:  2020-12-15       Impact factor: 41.582

7.  Regulation of efflux pump expression and drug resistance by the transcription factors Mrr1, Upc2, and Cap1 in Candida albicans.

Authors:  Sabrina Schubert; Katherine S Barker; Sadri Znaidi; Sabrina Schneider; Franziska Dierolf; Nico Dunkel; Malika Aïd; Geneviève Boucher; P David Rogers; Martine Raymond; Joachim Morschhäuser
Journal:  Antimicrob Agents Chemother       Date:  2011-03-14       Impact factor: 5.191

Review 8.  Candida albicans - Biology, molecular characterization, pathogenicity, and advances in diagnosis and control - An update.

Authors:  Maryam Dadar; Ruchi Tiwari; Kumaragurubaran Karthik; Sandip Chakraborty; Youcef Shahali; Kuldeep Dhama
Journal:  Microb Pathog       Date:  2018-02-16       Impact factor: 3.738

9.  The transcription factor Mrr1p controls expression of the MDR1 efflux pump and mediates multidrug resistance in Candida albicans.

Authors:  Joachim Morschhäuser; Katherine S Barker; Teresa T Liu; Julia BlaB-Warmuth; Ramin Homayouni; P David Rogers
Journal:  PLoS Pathog       Date:  2007-11       Impact factor: 6.823

10.  Quinone derivatives isolated from the endolichenic fungus Phialocephala fortinii are Mdr1 modulators that combat azole resistance in Candida albicans.

Authors:  Fei Xie; Wenqiang Chang; Ming Zhang; Ying Li; Wei Li; Hongzhuo Shi; Sha Zheng; Hongxiang Lou
Journal:  Sci Rep       Date:  2016-09-21       Impact factor: 4.379
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