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. 2014 Oct;58(10):6306-10.
doi: 10.1128/AAC.03668-14. Epub 2014 Aug 4.

The activity of glycopeptide antibiotics against resistant bacteria correlates with their ability to induce the resistance system

Min Jung Kwun  1 , Hee-Jeon Hong  2
Affiliations

The activity of glycopeptide antibiotics against resistant bacteria correlates with their ability to induce the resistance system

Min Jung Kwun et al. Antimicrob Agents Chemother. 2014 Oct.

Abstract

Glycopeptide antibiotics containing a hydrophobic substituent display the best activity against vancomycin-resistant enterococci, and they have been assumed to be poor inducers of the resistance system. Using a panel of 26 glycopeptide derivatives and the model resistance system in Streptomyces coelicolor, we confirmed this hypothesis at the level of transcription. Identification of the structural glycopeptide features associated with inducing the expression of resistance genes has important implications in the search for more effective antibiotic structures.

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Figures

FIG 1
FIG 1
Organization and regulation of the vancomycin resistance system (A) and the SigE system (B) in S. coelicolor.
FIG 2
FIG 2
Chemical structure of glycopeptide derivatives used in this study.
FIG 3
FIG 3
Induction of vanH and sigE transcription in S. coelicolor M600 in response to glycopeptide derivatives. Total RNAs were extracted from each sample and analyzed using qRT-PCR. The x axis indicates time (min) after addition of the treatment, and the y axis shows the fold change in expression relative to the level at time zero. For raw qRT-PCR data, see Tables S1 and S2 in the supplemental material. For the detailed experimental procedure, see the supplemental material.
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