Extended targeting potential and improved synthesis of Microcin C analogs as antibacterials

Gaston H.M. Vondenhoff, Svetlana Dubiley, Konstantin Severinov, Eveline Lescrinier, Jef Rozenski, Arthur Van Aerschot

Результат исследований: Вклад в журналСтатьярецензирование

21 Цитирования (Scopus)

Аннотация

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.

Язык оригиналаАнглийский
Страницы (с-по)5462-5467
Число страниц6
ЖурналBioorganic and Medicinal Chemistry
Том19
Номер выпуска18
DOI
СостояниеОпубликовано - 15 сент. 2011
Опубликовано для внешнего пользованияДа

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