Gomez Maria J, Neyfakh Alexander A
Center for Pharmaceutical Biotechnology (M/C 870), University of Illinois at Chicago, 900 S. Ashland Ave., Chicago, IL 60607, USA.
Antimicrob Agents Chemother. 2006 Nov;50(11):3562-7. doi: 10.1128/AAC.00579-06. Epub 2006 Aug 28.
Bacterial genes defining intrinsic resistance to antibiotics encode proteins that can be targeted by antibiotic potentiators. To find such genes, a transposon insertion library of Acinetobacter baylyi was screened with subinhibitory concentrations of various antibiotics to find supersusceptible mutants. A DNA microarray printer was used to replica plate 10,000 individual library clones to select mutants unable to grow at 1/10 the MICs of 12 different antibiotics. Transposon insertions in 11 genes were found to cause an eightfold or higher hypersusceptibility to at least one antibiotic. Most of the mutants identified exhibited hypersusceptibility to beta-lactam antibiotics. These included mutants with disruptions of genes encoding proteins involved in efflux (acrB and oprM) as well as genes pertaining to peptidoglycan synthesis and modification (ampD, mpl, and pbpG). However, disruptions of genes encoding proteins with seemingly unrelated functions (gph, argH, hisF, and ACIAD0795) can also render cells hypersusceptible to beta-lactam antibiotics. A knockout of gshA, involved in glutathione biosynthesis, enhanced the susceptibility to metronidazole, while a knockout of recD, involved in recombination and repair, made the bacteria hypersusceptible to ciprofloxacin. Disruption of acrB in Escherichia coli rendered the cells hypersusceptible to several antibiotics. However, knockout mutants of other homologous genes in E. coli showed no significant changes in antibiotic MICs, indicating that the intrinsic resistance genes are species specific.
定义细菌对抗生素固有抗性的基因编码的蛋白质可成为抗生素增效剂的作用靶点。为了找到此类基因,用亚抑制浓度的各种抗生素筛选拜氏不动杆菌的转座子插入文库,以寻找超敏感突变体。使用DNA微阵列打印机对10000个单独的文库克隆进行复制平板培养,以选择在12种不同抗生素的最低抑菌浓度(MIC)的1/10下无法生长的突变体。发现11个基因中的转座子插入导致对至少一种抗生素产生8倍或更高的超敏感性。鉴定出的大多数突变体对β-内酰胺类抗生素表现出超敏感性。这些包括编码参与外排的蛋白质的基因(acrB和oprM)以及与肽聚糖合成和修饰有关的基因(ampD、mpl和pbpG)发生破坏的突变体。然而,编码看似不相关功能的蛋白质的基因(gph、argH、hisF和ACIAD0795)的破坏也可使细胞对β-内酰胺类抗生素超敏感。参与谷胱甘肽生物合成的gshA基因敲除增强了对甲硝唑的敏感性,而参与重组和修复的recD基因敲除使细菌对环丙沙星超敏感。大肠杆菌中acrB的破坏使细胞对几种抗生素超敏感。然而,大肠杆菌中其他同源基因的敲除突变体在抗生素MIC方面没有显著变化,这表明固有抗性基因具有物种特异性。