Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity

Gonorrhea, which is caused by Neisseria gonorrhoeae, is the second most reported sexually transmitted infection worldwide. The increasing appearance of isolates that are resistant to approved therapeutics raises the concern that gonorrhea may become untreatable. Here, we serendipitously identified o...

Full description

Saved in:
Bibliographic Details
Main Authors: Jingbo Kan, Adrian Morales-Amador, Yozen Hernandez, Melinda A Ternei, Christophe Lemetre, Logan W Maclntyre, Nicolas Biais, Sean F Brady
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2025-05-01
Series:eLife
Subjects:
Online Access:https://elifesciences.org/articles/99281
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850108394164191232
author Jingbo Kan
Adrian Morales-Amador
Yozen Hernandez
Melinda A Ternei
Christophe Lemetre
Logan W Maclntyre
Nicolas Biais
Sean F Brady
author_facet Jingbo Kan
Adrian Morales-Amador
Yozen Hernandez
Melinda A Ternei
Christophe Lemetre
Logan W Maclntyre
Nicolas Biais
Sean F Brady
author_sort Jingbo Kan
collection DOAJ
description Gonorrhea, which is caused by Neisseria gonorrhoeae, is the second most reported sexually transmitted infection worldwide. The increasing appearance of isolates that are resistant to approved therapeutics raises the concern that gonorrhea may become untreatable. Here, we serendipitously identified oxydifficidin as a potent N. gonorrhoeae antibiotic through the observation of a Bacillus amyloliquefaciens contaminant in a lawn of N. gonorrhoeae. Oxydifficidin is active against both wild-type and multidrug-resistant N. gonorrhoeae. Its potent activity results from a combination of DedA-assisted uptake into the cytoplasm and the presence of an oxydifficidin-sensitive ribosomal protein L7/L12 (RplL). Our data indicate that oxydifficidin binds to the ribosome at a site that is distinct from other antibiotics and that L7/L12 is uniquely associated with its mode of action. This study opens a potential new avenue for addressing antibiotic resistant gonorrhea and underscores the possibility of identifying overlooked natural products from cultured bacteria, particularly those with activity against previously understudied pathogens.
format Article
id doaj-art-6d7e27b44cf34471a95e2b067d2e18e2
institution OA Journals
issn 2050-084X
language English
publishDate 2025-05-01
publisher eLife Sciences Publications Ltd
record_format Article
series eLife
spelling doaj-art-6d7e27b44cf34471a95e2b067d2e18e22025-08-20T02:38:22ZengeLife Sciences Publications LtdeLife2050-084X2025-05-011310.7554/eLife.99281Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivityJingbo Kan0https://orcid.org/0009-0006-1917-6577Adrian Morales-Amador1https://orcid.org/0000-0001-7944-308XYozen Hernandez2https://orcid.org/0000-0003-3349-8856Melinda A Ternei3Christophe Lemetre4Logan W Maclntyre5Nicolas Biais6https://orcid.org/0009-0004-6054-594XSean F Brady7https://orcid.org/0000-0001-5967-8586Laboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United States; Graduate Center, City University of New York, New York City, United States; Brooklyn College, City University of New York, New York, United StatesLaboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United StatesLaboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United StatesLaboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United StatesLaboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United StatesLaboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United StatesGraduate Center, City University of New York, New York City, United States; Brooklyn College, City University of New York, New York, United States; Laboratoire Jean Perrin, UMR 8237 Sorbonne Université/CNRS, Paris, FranceLaboratory of Genetically Encoded Small Molecules, The Rockefeller University, New York, United StatesGonorrhea, which is caused by Neisseria gonorrhoeae, is the second most reported sexually transmitted infection worldwide. The increasing appearance of isolates that are resistant to approved therapeutics raises the concern that gonorrhea may become untreatable. Here, we serendipitously identified oxydifficidin as a potent N. gonorrhoeae antibiotic through the observation of a Bacillus amyloliquefaciens contaminant in a lawn of N. gonorrhoeae. Oxydifficidin is active against both wild-type and multidrug-resistant N. gonorrhoeae. Its potent activity results from a combination of DedA-assisted uptake into the cytoplasm and the presence of an oxydifficidin-sensitive ribosomal protein L7/L12 (RplL). Our data indicate that oxydifficidin binds to the ribosome at a site that is distinct from other antibiotics and that L7/L12 is uniquely associated with its mode of action. This study opens a potential new avenue for addressing antibiotic resistant gonorrhea and underscores the possibility of identifying overlooked natural products from cultured bacteria, particularly those with activity against previously understudied pathogens.https://elifesciences.org/articles/99281Neisseria gonorrhoeaecell cultureantibiotics
spellingShingle Jingbo Kan
Adrian Morales-Amador
Yozen Hernandez
Melinda A Ternei
Christophe Lemetre
Logan W Maclntyre
Nicolas Biais
Sean F Brady
Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity
eLife
Neisseria gonorrhoeae
cell culture
antibiotics
title Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity
title_full Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity
title_fullStr Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity
title_full_unstemmed Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity
title_short Oxydifficidin, a potent Neisseria gonorrhoeae antibiotic due to DedA-assisted uptake and ribosomal protein RplL sensitivity
title_sort oxydifficidin a potent neisseria gonorrhoeae antibiotic due to deda assisted uptake and ribosomal protein rpll sensitivity
topic Neisseria gonorrhoeae
cell culture
antibiotics
url https://elifesciences.org/articles/99281
work_keys_str_mv AT jingbokan oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT adrianmoralesamador oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT yozenhernandez oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT melindaaternei oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT christophelemetre oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT loganwmaclntyre oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT nicolasbiais oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity
AT seanfbrady oxydifficidinapotentneisseriagonorrhoeaeantibioticduetodedaassisteduptakeandribosomalproteinrpllsensitivity