Zandomeni R, Mittleman B, Bunick D, Ackerman S, Weinmann R
Proc Natl Acad Sci U S A. 1982 May;79(10):3167-70. doi: 10.1073/pnas.79.10.3167.
The adenosine analog 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) and its mono- and triphosphate derivatives inhibit RNA polymerase II-specific transcription in an extract of whole HeLa cells. The analog does not inhibit RNA polymerase III-specific adenovirus VA RNA transcription in the whole cell extract. With purified RNA polymerase II under nonspecific transcription conditions, no effect on DRB could be detected. DRB is equally effective in inhibiting in vitro transcription from several of the adenovirus promoters and the human epsilon-globin gene. The inhibitory effects are in the order DRB greater than DRB monophosphate greater than DRB triphosphate. Thus DRB acts in vitro presumably on systems in which specific RNA polymerase II initiation of transcription occurs and with no detectable effect on premature termination. This will provide a suitable model for study of the molecular mechanism of action of DRB on transcription.
腺苷类似物5,6-二氯-1-β-D-呋喃核糖基苯并咪唑(DRB)及其单磷酸和三磷酸衍生物可抑制完整HeLa细胞提取物中RNA聚合酶II特异性转录。该类似物在全细胞提取物中不抑制RNA聚合酶III特异性腺病毒VA RNA转录。在非特异性转录条件下,纯化的RNA聚合酶II对DRB无影响。DRB在抑制来自几种腺病毒启动子和人ε-珠蛋白基因的体外转录方面同样有效。抑制作用顺序为DRB大于DRB单磷酸大于DRB三磷酸。因此,DRB在体外可能作用于发生特异性RNA聚合酶II转录起始的系统,且对过早终止无明显影响。这将为研究DRB对转录作用的分子机制提供一个合适的模型。