ArticleScientific reports2017
Microspectrofluorimetry to dissect the permeation of ceftazidime in Gram-negative bacteria.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 1 of them a synthesis that pooled it.
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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.
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Who cites it
12 citing papers in PubMed, 1 synthesis or guideline pooled it, 29 citations in OpenAlex.
- Pharmacokinetic-pharmacodynamic modeling using combined time-kill data for meropenem and colistin or polymyxin B combination effects inAntimicrobial agents and chemotherapy · 2026Pooled it
- Rapid profiling of polymyxin B susceptibility in Gram-negative bacteria with a novel polymyxin-derived fluorescent probe.Journal of advanced research · 2026Article
- Antechodynamics and Antechokinetics: Dynamics and Kinetics of Antibiotic Resistance Biomolecules.Biomolecules · 2025Review
- Cytoplasmic Accumulation and Permeability of Antibiotics in Gram Positive and Gram Negative Bacteria Visualized in Real-Time via a Fluorogenic Tagging Strategy.ACS chemical biology · 2024Article
- Cephalosporin translocation across enterobacterial OmpF and OmpC channels, a filter across the outer membrane.Communications biology · 2022Article
- Live-Cell Profiling of Penicillin-Binding Protein Inhibitors inACS infectious diseases · 2022Article
- Porins and small-molecule translocation across the outer membrane of Gram-negative bacteria.Nature reviews. Microbiology · 2020Review
- Fluoroquinolone-derived fluorescent probes for studies of bacterial penetration and efflux.MedChemComm · 2019Article
- Reversing resistance to counter antimicrobial resistance in the World Health Organisation's critical priority of most dangerous pathogens.Bioscience reports · 2019Review
- Article
- Translocation of small molecules through engineered outer-membrane channels from Gram-negative bacteria.The European physical journal. E, Soft matter · 2018Article
- Spectrofluorimetric quantification of antibiotic drug concentration in bacterial cells for the characterization of translocation across bacterial membranes.Nature protocols · 2018Article
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A main challenge in chemotherapy is to determine the in cellulo parameters modulating the drug concentration required for therapeutic action. It is absolutely urgent to understand membrane permeation and intracellular concentration of antibiotics in clinical isolates: passing the membrane barrier to reach the threshold concentration inside the bacterial periplasm or cytoplasm is the pivotal step of antibacterial activity. Ceftazidime (CAZ) is a key molecule of the combination therapy for treating resistant bacteria. We designed and synthesized different fluorescent CAZ derivatives (CAZ*, CAZ**) to dissect the early step of translocation-accumulation across bacterial membrane. Their activities were determined on E. coli strains and on selected clinical isolates overexpressing ß-lactamases. The accumulation of CAZ* and CAZ** were determined by microspectrofluorimetry and epifluorimetry. The derivatives were properly translocated to the periplasmic space when we permeabilize the outer membrane barrier. The periplasmic location of CAZ** was related to a significant antibacterial activity and with the outer membrane permeability. This study demonstrated the correlation between periplasmic accumulation and antibiotic activity. We also validated the method for approaching ß-lactam permeation relative to membrane permeability and paved the way for an original matrix for determining "Structure Intracellular Accumulation Activity Relationship" for the development of new therapeutic candidates.
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Registered trials
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 OpenQuestion graph.