ArticlePloS one2009
New antibiotic molecules: bypassing the membrane barrier of gram negative bacteria increases the activity of peptide deformylase inhibitors.
Article in PloS one, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Pharmacokinetics and tolerability of IDP-73152 mesylate after a single oral administration under fasted and fed conditions in healthy volunteers.Drug design, development and therapy · 2019Trial
- Compounds Containing 2,3-Bis(phenylamino) Quinoxaline Exhibit Activity Against Methicillin-Resistant Staphylococcus aureus, Enterococcus faecalis, and Their Biofilms.MicrobiologyOpen · 2024Article
- The antibacterial effect ofJournal of traditional and complementary medicine · 2022Article
- Nanotargeting of Resistant Infections with a Special Emphasis on the Biofilm Landscape.Bioconjugate chemistry · 2021Review
- Reversing resistance to counter antimicrobial resistance in the World Health Organisation's critical priority of most dangerous pathogens.Bioscience reports · 2019Review
- Reconstitution of Mammalian Enzymatic Deacylation Reactions in Live Bacteria Using Native Acylated Substrates.ACS synthetic biology · 2018Article
- Green Tea Seed Isolated Saponins Exerts Antibacterial Effects against Various Strains of Gram Positive and Gram Negative Bacteria, a Comprehensive StudyEvidence-based complementary and alternative medicine : eCAM · 2018Article
- Fluoroquinolone structure and translocation flux across bacterial membrane.Scientific reports · 2017Article
- Microspectrofluorimetry to dissect the permeation of ceftazidime in Gram-negative bacteria.Scientific reports · 2017Article
- A unique peptide deformylase platform to rationally design and challenge novel active compounds.Scientific reports · 2016Article
- Mutant Alleles of lptD Increase the Permeability of Pseudomonas aeruginosa and Define Determinants of Intrinsic Resistance to Antibiotics.Antimicrobial agents and chemotherapy · 2016Article
- Polyamino-Isoprenic Derivatives Block Intrinsic Resistance of P. aeruginosa to Doxycycline and Chloramphenicol In Vitro.PloS one · 2016Article
- Role of the Outer Membrane and Porins in Susceptibility of β-Lactamase-Producing Enterobacteriaceae to Ceftazidime-Avibactam.Antimicrobial agents and chemotherapy · 2015Article
- Effects of saponins against clinical E. coli strains and eukaryotic cell line.Journal of biomedicine & biotechnology · 2012Article
- Involvement of the efflux pumps in chloramphenicol selected strains of Burkholderia thailandensis: proteomic and mechanistic evidence.PloS one · 2011Article
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundMulti-drug resistant (MDR) bacteria have become a major concern in hospitals worldwide and urgently require the development of new antibacterial molecules. Peptide deformylase is an intracellular target now well-recognized for the design of new antibiotics. The bacterial susceptibility to such a cytoplasmic target primarily depends on the capacity of the compound to reach and accumulate in the cytosol. METHODOLOGY/PRINCIPAL
findingsTo determine the respective involvement of penetration (influx) and pumping out (efflux) mechanisms to peptide deformylase inhibitors (PDF-I) activity, the potency of various series was determined using various genetic contexts (efflux overproducers or efflux-deleted strains) and membrane permeabilizers. Depending on the structure of the tested molecules, two behaviors could be observed: (i) for actinonin the first PDF-I characterized, the AcrAB efflux system was the main parameter involved in the bacterial susceptibility, and (ii), for the latest PDF-Is such as the derivatives of 2-(5-bromo-1H-indol-3-yl)-N-hydroxyacetamide, the penetration through the membrane was a important limiting step. CONCLUSIONS/SIGNIFICANCE: Our results clearly show that the bacterial membrane plays a key role in modulating the antibacterial activity of PDF-Is. The bacterial susceptibility for these new antibacterial molecules can be improved by two unrelated ways in MDR strains: by collapsing the Acr efflux activity or by increasing the uptake rate through the bacterial membrane. The efficiency of the second method is associated with the nature of the compound.
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