MICROCIN C: BIOSYNTHESIS, MODE OF ACTION, AND POTENTIAL AS A LEAD IN ANTIBIOTICS DEVELOPMENT

被引：7
|
作者：
Vondenhoff, Gaston H. M. [1 ]
Van Aerschot, Arthur [1 ]
机构：
[1] Katholieke Univ Leuven, Med Chem Lab, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2011年 / 30卷 / 7-9期
关键词：
Microcin C; aminoacyl tRNA synthetase inhibitors; antibiotics; aminoacyl sulfamoyl adenosine; TRANSFER-RNA SYNTHETASE; ESCHERICHIA-COLI; ANTIMICROBIAL AGENTS; ADENYLATE ANALOGS; MATURATION; RESISTANCE; INHIBITORS; TRANSPORTER; PEPTIDASE; MECHANISM;
D O I：
10.1080/15257770.2011.583972
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The natural compound Microcin C (McC) is a Trojan home 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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页码：465 / 474
页数：10
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