Microcin C: Biosynthesis,Mode of Action,and Potential as a Lead in Antibiotics Development |
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Authors: | Mr Gaston H M Vondenhoff Arthur Van Aerschot |
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Institution: | Laboratory of Medicinal Chemistry, Rega Institute for Medical Research , Katholieke Universiteit Leuven , Leuven , Belgium |
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Abstract: | The natural compound Microcin C (McC) is a Trojan horse inhibitor of aspartyl tRNA synthetases endowed with strong antibacterial properties, in which a heptapeptide moiety is responsible for active transport of the inhibitory metabolite part into the bacterial cell. The intracellularly formed aspartyl AMP analogue carries a chemically more stable phosphoramidate linkage, in comparison to the labile aspartyl-adenylate, and in addition is esterified with a 3-aminopropyl moiety. Therefore, this compound can target aspartyl-tRNA synthetase. The biochemical production and secretion of McC, and the possibilities to develop new classes of antibiotics using the McC Trojan horse concept in combination with sulfamoylated adenosine analogues will be discussed briefly. |
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Keywords: | Microcin C aminoacyl tRNA synthetase inhibitors antibiotics aminoacyl sulfamoyl adenosine |
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