Domínguez J M, Martín J J
Departamento de Investigación, Glaxo Wellcome S.A. 28760-Tres Cantos, Madrid, Spain.
Antimicrob Agents Chemother. 1998 Sep;42(9):2279-83. doi: 10.1128/AAC.42.9.2279.
The target for sordarins in Candida albicans has been elucidated. Kinetic experiments of sordarin inhibition as well as displacement experiments showed that the formation of a sordarin-target complex follows a reversible mechanism. Binding of tritiated drug to the target is enhanced in the presence of ribosomes. Isolation of the target by classical protein purification methods has allowed us to identify it as elongation factor 2. This is in agreement with the nature of sordarin derivatives as specific inhibitors of the elongation cycle within protein synthesis in yeasts.
已阐明了念珠菌中梭链孢酸的作用靶点。梭链孢酸抑制的动力学实验以及置换实验表明,梭链孢酸 - 靶点复合物的形成遵循可逆机制。在核糖体存在的情况下,氚标记药物与靶点的结合增强。通过经典蛋白质纯化方法分离靶点使我们能够将其鉴定为延伸因子2。这与梭链孢酸衍生物作为酵母蛋白质合成中延伸循环的特异性抑制剂的性质相符。