Carrano Lucia, Alifano Pietro, Corti Emiliana, Bucci Cecilia, Donadio Stefano
Biosearch Italia, via R. Lepetit 34, 21040 Gerenzano, VA, Italy.
Biochem Biophys Res Commun. 2003 Mar 7;302(2):219-25. doi: 10.1016/s0006-291x(03)00131-1.
In this study we describe BI-K0058, a new inhibitor of the transcription-termination factor Rho belonging to a different chemical class from bicyclomycin, the only known antibiotic acting on Rho. BI-K0058 inhibits the poly(C)-dependent ATPase activity of Rho with an IC(50) of 25 microM as well as in vitro transcription-termination of two natural substrates, the Salmonella enterica hisG cistron and the f1 phage intergenic region. BI-K0058 does not affect photolabeling of Rho by ATP. The results of gel mobility shift experiments with a natural RNA substrate demonstrate that BI-K0058 inhibits the formation of the ATP-independent high affinity Rho-RNA complex.
在本研究中，我们描述了BI-K0058，一种转录终止因子Rho的新型抑制剂，它与双环霉素属于不同的化学类别，双环霉素是唯一已知的作用于Rho的抗生素。BI-K0058抑制Rho的聚（C）依赖性ATP酶活性，IC（50）为25 microM，同时也抑制两种天然底物（肠炎沙门氏菌hisG顺反子和f1噬菌体基因间区域）的体外转录终止。BI-K0058不影响ATP对Rho的光标记。使用天然RNA底物进行的凝胶迁移率变动实验结果表明，BI-K0058抑制了不依赖ATP的高亲和力Rho-RNA复合物的形成。
