一种新型转录终止因子Rho的抑制剂。

A new inhibitor of the transcription-termination factor Rho.

作者信息

Carrano Lucia, Alifano Pietro, Corti Emiliana, Bucci Cecilia, Donadio Stefano

机构信息

Biosearch Italia, via R. Lepetit 34, 21040 Gerenzano, VA, Italy.

出版信息

Biochem Biophys Res Commun. 2003 Mar 7;302(2):219-25. doi: 10.1016/s0006-291x(03)00131-1.

DOI:10.1016/s0006-291x(03)00131-1

PMID:12604334

Abstract

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.

摘要

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。