Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis

Abstract To replicate and cause disease, Mycobacterium tuberculosis secretes siderophores called mycobactins to scavenge iron from the human host. Two closely related transporters, MmpL4 and MmpL5, are required for mycobactin secretion and drug efflux. In clinical strains, overproduction of MmpL5 co...

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Main Authors: Jennifer C. Earp, Alisa A. Garaeva, Virginia Meikle, Michael Niederweis, Markus A. Seeger
Format: Article
Language:English
Published: Nature Portfolio 2025-02-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-025-56888-6
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author Jennifer C. Earp
Alisa A. Garaeva
Virginia Meikle
Michael Niederweis
Markus A. Seeger
author_facet Jennifer C. Earp
Alisa A. Garaeva
Virginia Meikle
Michael Niederweis
Markus A. Seeger
author_sort Jennifer C. Earp
collection DOAJ
description Abstract To replicate and cause disease, Mycobacterium tuberculosis secretes siderophores called mycobactins to scavenge iron from the human host. Two closely related transporters, MmpL4 and MmpL5, are required for mycobactin secretion and drug efflux. In clinical strains, overproduction of MmpL5 confers resistance towards bedaquiline and clofazimine, key drugs to combat multidrug resistant tuberculosis. Here, we present cryogenic-electron microscopy structures of MmpL4 and identify a mycobactin binding site, which is accessible from the cytosol and also required for bedaquiline efflux. An unusual coiled-coil domain predicted to extend 130 Å into the periplasm is essential for mycobactin and bedaquiline efflux by MmpL4 and MmpL5. The mycobacterial acyl carrier protein MbtL forms a complex with MmpL4, indicating that mycobactin synthesis and export are coupled. Thus, MmpL4 and MmpL5 constitute the core components of a unique multi-subunit machinery required for iron acquisition and drug efflux by M. tuberculosis.
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spelling doaj-art-a3e5416cc44b4b2d8b5bbbe753a5308e2025-08-20T02:59:35ZengNature PortfolioNature Communications2041-17232025-02-0116111310.1038/s41467-025-56888-6Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosisJennifer C. Earp0Alisa A. Garaeva1Virginia Meikle2Michael Niederweis3Markus A. Seeger4Institute of Medical Microbiology, University of ZurichInstitute of Medical Microbiology, University of ZurichDepartment of Microbiology, University of Alabama at BirminghamDepartment of Microbiology, University of Alabama at BirminghamInstitute of Medical Microbiology, University of ZurichAbstract To replicate and cause disease, Mycobacterium tuberculosis secretes siderophores called mycobactins to scavenge iron from the human host. Two closely related transporters, MmpL4 and MmpL5, are required for mycobactin secretion and drug efflux. In clinical strains, overproduction of MmpL5 confers resistance towards bedaquiline and clofazimine, key drugs to combat multidrug resistant tuberculosis. Here, we present cryogenic-electron microscopy structures of MmpL4 and identify a mycobactin binding site, which is accessible from the cytosol and also required for bedaquiline efflux. An unusual coiled-coil domain predicted to extend 130 Å into the periplasm is essential for mycobactin and bedaquiline efflux by MmpL4 and MmpL5. The mycobacterial acyl carrier protein MbtL forms a complex with MmpL4, indicating that mycobactin synthesis and export are coupled. Thus, MmpL4 and MmpL5 constitute the core components of a unique multi-subunit machinery required for iron acquisition and drug efflux by M. tuberculosis.https://doi.org/10.1038/s41467-025-56888-6
spellingShingle Jennifer C. Earp
Alisa A. Garaeva
Virginia Meikle
Michael Niederweis
Markus A. Seeger
Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis
Nature Communications
title Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis
title_full Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis
title_fullStr Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis
title_full_unstemmed Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis
title_short Structural basis of siderophore export and drug efflux by Mycobacterium tuberculosis
title_sort structural basis of siderophore export and drug efflux by mycobacterium tuberculosis
url https://doi.org/10.1038/s41467-025-56888-6
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