Evidence map›Paper›PMID 39960147›Full record

ArticleChemMedChem2025

Fast Release of Carboxylic Acid inside Cells.

Pascal Moser, Renaud Zelli, Leandro J Dos Santos, Mickaël Henry, Kevin Sanchez-Garcia, Yvan Caspar, Florian C Marro, Benoit Chovelon, Jaione Saez Cabodevilla, Sandrine Ollagnier de Choudens and 2 more

Abstract read
In one paragraph

Article in ChemMedChem, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Pascal MoserUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.
Renaud ZelliUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.
Leandro J Dos SantosUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.
Mickaël HenryUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.
Kevin Sanchez-GarciaLaboratoire de Bactériologie-Hygiène Hospitalière, CHU Grenoble Alpes, CS10317 38043, Grenoble cedex 9, France.
Yvan CasparLaboratoire de Bactériologie-Hygiène Hospitalière, CHU Grenoble Alpes, CS10317 38043, Grenoble cedex 9, France.
Florian C MarroBiozentrum, University of Basel, Basel, 4056, Switzerland.
Benoit ChovelonUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.
Jaione Saez CabodevillaUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.
Sandrine Ollagnier de ChoudensUniv. Grenoble Alpes, CEA, CNRS, LCBM, UMR 5249, 38000, Grenoble, France.
Eric FaudryUniv. Grenoble Alpes, CNRS, CEA, IBS, Bact.Path. & Cel. Resp., 38000, Grenoble, France.
Yung-Sing WongUniv. Grenoble Alpes, CNRS, DPM, 38000, Grenoble, France.ORCID https://orcid.org/0000-0003-1038-9681

Funding

Labex ARCANE programs ANR-17-EURE-0003University Grenoble Alpes
6 · The paper itself

Abstract

Delivering carboxylic acid functions into cells is challenging due to their poor permeability across lipophilic membranes at physiological pH, where they are ionized. Masking carboxylic acids as esters improves cell entry, but once inside the cell, its rapid release is essential to maintain spatiotemporal control which can be beneficial for therapeutic and diagnostic applications. This study evaluates the 2-hydroxyethyl-dithio-benzyl ester functional group which undergoes selective and rapid cleavage of the disulfide bond by thioredoxin (Trx), triggering rapid self-immolation of the thio-benzyl ester releasing the carboxylic acid. Fluorescence-based assays using the pro-fluorescent BODIPY structure have demonstrated the rapid intracellular release of carboxylic acids within minutes in both eukaryotic and prokaryotic cells. The approach was tested on antibiotics, and among them, levofloxacin ester prodrug, having the 2-hydroxyethyl-dithio-benzyl ester functional group, showed significantly enhanced antimicrobial activity against resistant and intracellular bacteria compared to its methyl ester analogue.

Indexed as

Anti-Bacterial AgentsCarboxylic AcidsLevofloxacinProdrugsBoron CompoundsFluorescent DyesHumansMicrobial Sensitivity TestsMolecular StructureStructure-Activity Relationship4,4-difluoro-4-bora-3a,4a-diaza-s-indaceneAnti-Bacterial AgentsBoron CompoundsCarboxylic AcidsFluorescent DyesLevofloxacinProdrugs

Identifiers

PMID39960147
PMCPMC12058233

What Socratic holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.