Structural insights into fosfomycin efflux by a streptococcal ABC transporter

ABSTRACT Gram-positive bacteria encode a broad array of ABC transporters that mediate substrate translocation across the cell membrane, with some contributing to their survival under environmental stresses such as antimicrobial exposure. While several of these transporters have been shown to exhibit multidrug efflux activity, the functional roles of many others remain unknown. Here, using an efflux pump screen in the opportunistic human pathogen Streptococcus pneumoniae , we identified a previously uncharacterized type IV ABC transporter (FoeAB) that confers resistance to the antibiotic fosfomycin. We show that purified FoeAB mediates fosfomycin transport in a liposome-reconstituted system and provide evidence that it functions as a multidrug efflux pump with substrate preferences distinct from those of known efflux pumps. Furthermore, we present cryogenic electron microscopy (cryo-EM) structures of FoeAB in inward- and outward-facing states, which reveal conformational changes associated with nucleotide binding and identify residues important for substrate transport. Collectively, these findings expand the known repertoire of antibiotic-exporting ABC transporters in Gram-positive bacteria and provide structural insight into its transport mechanism. SIGNIFICANCE Efflux pumps often play major roles in antibiotic resistance in clinically important pathogens, yet many of these transporters remain poorly defined. In this study, we identify and mechanistically characterize FoeAB, a previously unrecognized type IV ABC transporter in streptococcal species that mediates efflux of the antibiotic fosfomycin. By combining functional assays with structural studies of FoeAB in multiple conformational states, we propose a model for how this transporter recognizes its substrate and harnesses nucleotide-driven conformational changes to mediate substrate export. Our findings point to a previously underappreciated efflux capabilities in Gram-positive bacteria, highlighting the need for better characterization of membrane transporters to clarify their roles in bacterial physiology and drug resistance.

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Journal
Proceedings of the National Academy of Sciences
Published
2026-08-28
DOI
https://doi.org/10.1073/pnas.2535933123
Primary Topic
Drug Transport and Resistance Mechanisms
Type
article
Field-Weighted Citation Impact
0.00

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article

Structural insights into fosfomycin efflux by a streptococcal ABC transporter

Kunihiko Nishino, Mikio Tanabe, Keiichi Namba, Toshio Moriya et al.
Proceedings of the National Academy of Sciences
Drug Transport and Resistance Mechanisms
article

Structural insights into fosfomycin efflux by a streptococcal ABC transporter

Kunihiko Nishino, Mikio Tanabe, Keiichi Namba, Toshio Moriya, Junso Fujita, Kazuo Harada, Daisuke Takaya, Atsushi Taguchi, Kaori Fukuzawa
article en

Abstract

ABSTRACT Gram-positive bacteria encode a broad array of ABC transporters that mediate substrate translocation across the cell membrane, with some contributing to their survival under environmental stresses such as antimicrobial exposure. While several of these transporters have been shown to exhibit multidrug efflux activity, the functional roles of many others remain unknown. Here, using an efflux pump screen in the opportunistic human pathogen Streptococcus pneumoniae , we identified a previously uncharacterized type IV ABC transporter (FoeAB) that confers resistance to the antibiotic fosfomycin. We show that purified FoeAB mediates fosfomycin transport in a liposome-reconstituted system and provide evidence that it functions as a multidrug efflux pump with substrate preferences distinct from those of known efflux pumps. Furthermore, we present cryogenic electron microscopy (cryo-EM) structures of FoeAB in inward- and outward-facing states, which reveal conformational changes associated with nucleotide binding and identify residues important for substrate transport. Collectively, these findings expand the known repertoire of antibiotic-exporting ABC transporters in Gram-positive bacteria and provide structural insight into its transport mechanism. SIGNIFICANCE Efflux pumps often play major roles in antibiotic resistance in clinically important pathogens, yet many of these transporters remain poorly defined. In this study, we identify and mechanistically characterize FoeAB, a previously unrecognized type IV ABC transporter in streptococcal species that mediates efflux of the antibiotic fosfomycin. By combining functional assays with structural studies of FoeAB in multiple conformational states, we propose a model for how this transporter recognizes its substrate and harnesses nucleotide-driven conformational changes to mediate substrate export. Our findings point to a previously underappreciated efflux capabilities in Gram-positive bacteria, highlighting the need for better characterization of membrane transporters to clarify their roles in bacterial physiology and drug resistance.

Proceedings of the National Academy of SciencesVol. 123(35)
High Energy Accelerator Research Organization (JP), Ube Frontier University (JP), Sanken Electric (Japan) (JP), Futaba (Japan) (JP), Osaka University of Pharmaceutical Sciences (JP), The University of Osaka (JP)
Takeda Science Foundation, Institute for Fermentation, Osaka, Japan Agency for Medical Research and Development, Noda Institute for Scientific Research, Japan Society for the Promotion of Science
Life in Land
Openalex Percentile: Top 34%
Drug Transport and Resistance Mechanisms
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