title: The activity of glycopeptide antibiotics against resistant bacteria correlates with their ability to induce the resistance system.
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.
authors.affiliation: Department of Biochemistry, University of Cambridge, Cambridge, United Kingdom.
authors.forename: Min Jung
authors.initials: MJ
authors.lastname: Kwun
authors.affiliation: Department of Biochemistry, University of Cambridge, Cambridge, United Kingdom hh309@cam.ac.uk.
authors.forename: Hee-Jeon
authors.initials: HJ
authors.lastname: Hong
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D006020:Glycopeptides / Q000494:pharmacology*; D048372:Streptomyces coelicolor / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D006020:Glycopeptides
references.citation: J Med Chem. 1989 Nov;32(11):2450-60
references.pmid: 2530352
references.citation: Mol Microbiol. 2006 Feb;59(3):923-35
references.pmid: 16420361
references.citation: Biochemistry. 1991 Oct 29;30(43):10408-15
references.pmid: 1931965
references.citation: Biochemistry. 2008 Mar 25;47(12):3822-31
references.pmid: 18302341
references.citation: Antimicrob Agents Chemother. 2010 Jul;54(7):2814-8
references.pmid: 20404117
references.citation: Antimicrob Agents Chemother. 1996 Oct;40(10):2291-5
references.pmid: 8891132
references.citation: Mol Microbiol. 2004 May;52(4):1107-21
references.pmid: 15130128
references.citation: J Bacteriol. 1996 Mar;178(5):1302-9
references.pmid: 8631706
references.citation: Biochemistry. 2001 Apr 17;40(15):4745-55
references.pmid: 11294642
references.citation: Antimicrob Agents Chemother. 2013 Sep;57(9):4470-80
references.pmid: 23836175
references.citation: J Am Chem Soc. 2005 Aug 3;127(30):10747-52
references.pmid: 16045364
references.citation: Nat Chem Biol. 2010 May;6(5):327-9
references.pmid: 20383152
references.citation: J Biol Chem. 2005 Apr 1;280(13):13055-61
references.pmid: 15632111
references.citation: J Am Chem Soc. 2002 Aug 7;124(31):9064-5
references.pmid: 12149006
references.citation: Mol Microbiol. 2002 Jun;44(5):1199-1211
references.pmid: 12068806
references.citation: BMC Genomics. 2011 May 11;12:226
references.pmid: 21569315
references.citation: J Antibiot (Tokyo). 1989 Jan;42(1):63-72
references.pmid: 2921228
references.citation: Antimicrob Agents Chemother. 2012 Apr;56(4):1784-96
references.pmid: 22232274
references.citation: Mol Microbiol. 1996 Jul;21(1):33-44
references.pmid: 8843432
references.citation: FEMS Microbiol Lett. 2000 Feb 15;183(2):209-14
references.pmid: 10675585