Advances in methods and concepts provide new insight into antibiotic fluxes across the bacterial membrane DOI Creative Commons
Julia Vergalli, Matthieu Réfrégiers, Paolo Ruggerone

et al.

Communications Biology, Journal Year: 2024, Volume and Issue: 7(1)

Published: Nov. 14, 2024

The sophisticated envelope of Gram-negative bacteria modulates the uptake small molecules in a side-chain-sensitive manner. Despite intensive theoretical and experimental investigations, general set pathways underpinning antibiotic has not been identified. This manuscript discusses passive influx versus active efflux antibiotics, considering responsible membrane proteins transported molecules. Recent methods have analyzed drug transport across bacterial order to understand their activity. combination vitro, cellulo silico shed light on key, mainly electrostatic, interactions between molecule surface, porins transporters during permeation. A key factor is relationship dose an compound near its target antibacterial activity critical early window. Today, methodology breakthroughs provide fruitful tools precisely dissect transport, identify steps resistance associated with impermeability efflux, highlight parameters generate more effective drugs. controls accumulation via mechanisms. article recent cellulo, highlighting "drug-transporters" dialogues proposes new perspectives overcome resistance.

Language: Английский

Molecular epidemiology and β-lactam resistance mechanisms of Enterobacter cloacae complex isolates obtained from bloodstream infections, Kyoto, Japan DOI Creative Commons

Akihiko Matsuo,

Yasufumi Matsumura, Keiichiro Mori

et al.

Microbiology Spectrum, Journal Year: 2025, Volume and Issue: unknown

Published: March 10, 2025

ABSTRACT The Enterobacter cloacae complex (ECC) comprises multiple species that require genomic analysis for precise identification. They produce inducible AmpC β-lactamase and may carry acquired β-lactamases, which are responsible cefotaxime cefepime resistance. To determine the molecular epidemiology, antimicrobial resistance, β-lactam resistance mechanisms of ECC, we conducted whole-genome sequencing analysis, susceptibility testing, mutation on bloodstream ECC isolates from patients in Kyoto, Japan. In 194 isolates, 13 six unnamed taxa were identified, with xiangfangensis (36%) being most common. A total 38% nonsusceptible to presented relatively high nonsusceptibility rates all agents tested. Among different species, hoffmannii highest both β-lactams non-β-lactams. cefotaxime-nonsusceptible 16% harbored genes encoding extended-spectrum β-lactamases (ESBLs), carbapenemase, and/or plasmid-mediated AmpC, ampC derepression was predominant mechanism remaining isolates. prevalent sequence types (STs) cefotaxime-susceptible different, although some STs shared by groups. Cefepime detected 7% associated E. ST78 ST93, ESBLs. Sixty-four mutants, experimentally obtained eight had various ampD mutations, 42% 99% mutants piperacillin/tazobactam, respectively, indicating risks use these antimicrobials. Continuous surveillance via phenotypic analyses is needed combat ECC. IMPORTANCE a group pathogenic bacteria cause nosocomial infections. produces chromosomal treatment failure despite initial third-generation cephalosporins selected -derepressed mutants. challenges identification have complicated our understanding selection appropriate treatment. this study, performed phenotypic, sequencing, among infections molecular-based third-/fourth-generation cephalosporins, specific clones contribute acquisition fourth-generation cephalosporin ampC- derepressed These data will help elucidate local epidemiology guide therapy infection control strategies ECC-related

Language: Английский

Citations

0

A Review of In Silico and In Vitro Approaches in the Fight Against Carbapenem‐Resistant Enterobacterales DOI Creative Commons

Muhammad Absar,

Abdul Rahman Zaidah, Amer Mahmood

et al.

Journal of Clinical Laboratory Analysis, Journal Year: 2025, Volume and Issue: unknown

Published: April 9, 2025

ABSTRACT Objectives The rise in carbapenem‐resistant Enterobacterales (CRE) has reinforced the global quest for developing effective therapeutics. Traditional drug discovery approaches have been inadequate overcoming this challenge due to their resource and time constraints. Methods English literature was searched by structured queries related our review between January 1, 2020, December 31, 2024. Results key resistance mechanisms CRE, such as enzymatic hydrolysis, decreased permeability, efflux pump overexpression, examined review. Computational technologies become pivotal discovering novel antimicrobial agents with improved accuracy efficiency. Besides this, highlights advances structure‐ ligand‐based identifying potential drugs against CRE. Recent studies demonstrating use of silico techniques develop targeted CRE also explored. Moreover, underscores significance integrating both vitro counter Enterobacterales, supported latest studies. However, these promising computational a few major drawbacks, lack standardized parameterization, potentially false positives, complexity clinical translations. regulatory barriers restrict progress new antimicrobials market approval. Conclusion inhibitor is gaining popularity, it can be expedited refining them reliable validation. innovative hybrid need hour tackle mitigate threat resistance.

Language: Английский

Citations

0

Advances in methods and concepts provide new insight into antibiotic fluxes across the bacterial membrane DOI Creative Commons
Julia Vergalli, Matthieu Réfrégiers, Paolo Ruggerone

et al.

Communications Biology, Journal Year: 2024, Volume and Issue: 7(1)

Published: Nov. 14, 2024

The sophisticated envelope of Gram-negative bacteria modulates the uptake small molecules in a side-chain-sensitive manner. Despite intensive theoretical and experimental investigations, general set pathways underpinning antibiotic has not been identified. This manuscript discusses passive influx versus active efflux antibiotics, considering responsible membrane proteins transported molecules. Recent methods have analyzed drug transport across bacterial order to understand their activity. combination vitro, cellulo silico shed light on key, mainly electrostatic, interactions between molecule surface, porins transporters during permeation. A key factor is relationship dose an compound near its target antibacterial activity critical early window. Today, methodology breakthroughs provide fruitful tools precisely dissect transport, identify steps resistance associated with impermeability efflux, highlight parameters generate more effective drugs. controls accumulation via mechanisms. article recent cellulo, highlighting "drug-transporters" dialogues proposes new perspectives overcome resistance.

Language: Английский

Citations

2