Strategies for bypassing the membrane barrier in multidrug resistant Gram-negative bacteria

被引：185

作者：

Bolla, Jean-Michel ^{[1
,2
]}

Alibert-Franco, Sandrine ^{[1
,2
,3
]}

Handzlik, Jadwiga ^{[3
,4
]}

Chevalier, Jacqueline ^{[1
,2
]}

Mahamoud, Abdallah ^{[1
,2
]}

Boyer, Gerard ^{[1
,2
,5
]}

Kiec-Kononowicz, Katarzyna ^{[3
,4
]}

Pages, Jean-Marie ^{[1
,2
,3
]}

机构：

[1] Univ Mediterranee, Fac Med, UMR MD1, F-13385 Marseille 05, France

[2] Univ Mediterranee, Fac Pharm, UMR MD1, F-13385 Marseille 05, France

[3] COST Act BM0701 ATENS, Brusells, Belgium

[4] Jagiellonian Univ, Coll Med, Dept Technol & Biotechnol Drugs, Krakow, Poland

[5] Univ Paul Cezanne, UMR CNRS 6263, Marseille, France

来源：

FEBS LETTERS | 2011年 / 585卷 / 11期

关键词：

Antibiotic; Bacterial efflux pump; Chemosensitizer; Drug transporter; Efflux pump inhibitor; Gram-negative bacteria; Lipopolysaccharide; MDR bacteria; Membrane permeability; Natural compound; Porin; Selectivity; EFFLUX PUMP INHIBITORS; ANTIMICROBIAL DRUG SUSCEPTIBILITY; 5-ARYLIDENE AROMATIC DERIVATIVES; PSEUDOMONAS-AERUGINOSA; ESCHERICHIA-COLI; ANTIMYCOBACTERIAL ACTIVITY; CRYSTAL-STRUCTURE; ACRB; MECHANISMS; 1-(1-NAPHTHYLMETHYL)-PIPERAZINE;

D O I：

10.1016/j.febslet.2011.04.054

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In Gram-negative bacteria, the envelope is a sophisticated barrier protecting the cell against external toxic compounds. Membrane transporters, e. g., porins or efflux pumps, are main filters regulating the internal accumulation of various hydrophilic molecules. Regarding bacterial susceptibility towards antibacterial agents, membrane permeability is part of the early bacterial defense. The bacterium manages the translocation process, influx and efflux, to control the intracellular concentration of various molecules. Antibiotics and biocides are substrates of these mechanisms and the continuing emergence of multidrug resistant isolates is a growing worldwide health concern. Different strategies could be proposed to bypass the bacterial membrane barrier, comprising influx and efflux mechanisms, in order to restore the activity of antibiotics against resistant bacteria. (C) 2011 Federation of European Biochemical Societies. Published by Elsevier B. V. All rights reserved.

引用

页码：1682 / 1690

页数：9

共 110 条

[1]

Abeylath SC, 2008, EXPERT OPIN DRUG DEL, V5, P931, DOI [10.1517/17425247.5.9.931, 10.1517/17425247.5.9.931 ]

[2] Molecular mechanisms of antibacterial multidrug resistance [J].