Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
Bioorg Med Chem. 2011 Sep 15;19(18):5462-7. doi: 10.1016/j.bmc.2011.07.052. Epub 2011 Aug 3.
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.
微菌素 C（McC）（1）是某些大肠杆菌菌株产生的一种强效抗菌化合物。McC 通过木马机制发挥作用：它通过 YejABEF 转运蛋白的功能被主动摄取到敏感细胞内，然后被细胞氨肽酶处理。经过处理的 McC（2）是一种不可水解的天冬氨酰-腺苷酸类似物，可抑制天冬氨酰-tRNA 合成酶（AspRS）。本文描述了一种新的合成方法，可在可接受的量下生产各种 McC 类似物。使用该合成方法，合成了具有不同靶特异性的多种化合物。还使用这些化合物确定了 YejABEF 转运蛋白的进一步特性。
