Title: Extended targeting potential and improved synthesis of Microcin C analogs as antibacterials
Authors: Vondenhoff, Gaston H. M
Dubiley, Svetlana
Severinov, Konstantin
Lescrinier, Eveline
Rozenski, Jef
Van Aerschot, Arthur # ×
Issue Date: Sep-2011
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:19 issue:18 pages:5462-5467
Abstract: Microcin C (McC) (1) is a potent antibacterial compound produced by some Escherichia coli strains. McC functions through a Trojan-Horse mechanism: it is actively taken up inside a sensitive cell through the function of the YejABEF-transporter and then processed by cellular aminopeptidases. Processed McC (2) is a non-hydrolysable aspartyl-adenylate analog that inhibits aspartyl-tRNA synthetase (AspRS). A new synthesis is described that allows for the production of a wide variety of McC analogs in acceptable amounts. Using this synthesis a number of diverse compounds was synthesized with altered target specificity. Further characteristics of the YejABEF transporters were determined using these compounds. (C) 2011 Elsevier Ltd. All rights reserved.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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