The Heterodimeric ABC Transporter EfrCD Mediates Multidrug Efflux in Enterococcus faecalis.
Author(s)
Type
Journal Article
Abstract
Nosocomial infections with Enterococcus faecalis are an emerging health problem. However, drug efflux pumps contributing to intrinsic drug resistance are poorly studied in this Gram-positive pathogen. In this study, we functionally investigated seven heterodimeric ABC transporters of E. faecalis that are annotated as drug efflux pumps. Deletion of ef0789-ef0790 on the chromosome of E. faecalis resulted in increased susceptibility to daunorubicin, doxorubicin, ethidium, and Hoechst 33342, and the corresponding transporter was named EfrCD. Unexpectedly, the previously described heterodimeric multidrug ABC transporter EfrAB contributes marginally to drug efflux in the endogenous context of E. faecalis In contrast, heterologous expression in Lactococcus lactis revealed that EfrAB, EfrCD, and the product of ef2226-ef2227 (EfrEF) mediate the efflux of fluorescent substrates and confer resistance to multiple dyes and drugs, including fluoroquinolones. Four of seven transporters failed to exhibit drug efflux activity for the set of drugs and dyes tested, even upon overexpression in L. lactis Since all seven transporters were purified as heterodimers after overexpression in L. lactis, a lack of drug efflux activity is not attributed to poor expression or protein aggregation. Reconstitution of the purified multidrug transporters EfrAB, EfrCD, and EfrEF in proteoliposomes revealed functional coupling between ATP hydrolysis and drug binding. Our analysis creates an experimental basis for the accurate prediction of drug efflux transporters and indicates that many annotated multidrug efflux pumps might be incapable of drug transport and thus might fulfill other physiological functions in the cell.
Date Issued
2016-09-01
Date Acceptance
2016-06-20
Citation
Antimicrobial Agents and Chemotherapy, 2016, 60 (9), pp.5400-5411
ISSN
0066-4804
Publisher
American Society for Microbiology
Start Page
5400
End Page
5411
Journal / Book Title
Antimicrobial Agents and Chemotherapy
Volume
60
Issue
9
Copyright Statement
© 2016 Hürlimann et al. This is an open-access article distributed under
the terms of the Creative Commons Attribution 4.0 International license.
the terms of the Creative Commons Attribution 4.0 International license.
License URL
Identifier
PII: AAC.00661-16
Subjects
ATP-Binding Cassette Transporters
Adenosine Triphosphate
Amino Acid Sequence
Anti-Bacterial Agents
Bacterial Proteins
Base Sequence
Benzimidazoles
Biological Transport
Chromosomes, Bacterial
Daunorubicin
Doxorubicin
Enterococcus faecalis
Ethidium
Fluoroquinolones
Gene Expression
Genetic Loci
Lactococcus lactis
Protein Binding
Protein Conformation, alpha-Helical
Protein Conformation, beta-Strand
Protein Interaction Domains and Motifs
Protein Multimerization
Proteolipids
Recombinant Proteins
Sequence Deletion
Transgenes
Publication Status
Published