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二氯-β-D-呋喃核糖基苯并咪唑的作用机制:对体外转录的影响

Mechanism of action of dichloro-beta-D-ribofuranosylbenzimidazole: effect on in vitro transcription.

作者信息

Zandomeni R, Mittleman B, Bunick D, Ackerman S, Weinmann R

出版信息

Proc Natl Acad Sci U S A. 1982 May;79(10):3167-70. doi: 10.1073/pnas.79.10.3167.

DOI:10.1073/pnas.79.10.3167
PMID:6954467
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC346375/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/83e2349bd760/pnas00449-0113-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/78b88404a425/pnas00449-0112-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/5102afc58b1c/pnas00449-0113-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/83e2349bd760/pnas00449-0113-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/78b88404a425/pnas00449-0112-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/5102afc58b1c/pnas00449-0113-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a5c/346375/83e2349bd760/pnas00449-0113-b.jpg

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Mechanism of action of dichloro-beta-D-ribofuranosylbenzimidazole: effect on in vitro transcription.二氯-β-D-呋喃核糖基苯并咪唑的作用机制:对体外转录的影响
Proc Natl Acad Sci U S A. 1982 May;79(10):3167-70. doi: 10.1073/pnas.79.10.3167.
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本文引用的文献

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Short capped hnRNA precursor chains in HeLa cells: continued synthesis in the presence of 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole.
细胞核分级分离揭示了数千种与活跃基因相邻的染色质结合非编码RNA。
Cell Rep. 2015 Aug 18;12(7):1089-98. doi: 10.1016/j.celrep.2015.07.033. Epub 2015 Aug 6.
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Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia cells.RNA聚合酶II抑制剂在靶向休眠白血病细胞中的疗效。
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