A transcription inhibitor specific for unwound DNA in RNA polymerase-promoter open complexes.
A transcription inhibitor specific for unwound DNA in RNA polymerase-promoter open complexes.
复制标题
一种转录抑制剂，专门针对 RNA 聚合酶启动子开放复合物中解开的 DNA。
DOI：
10.1073/pnas.90.17.8140
复制
发表时间：
1993
影响因子：
11.1
通讯作者：
Sigman,DS
中科院分区：
文献类型：
--
作者：
Mazumder,A;Perrin,DM;Watson,KJ;Sigman,DS
The kinetically component open complexes formed at prokaryotic and eukaryotic transcription start sites are efficiently nicked by the chemical nuclease activity of the 2:1 1,10-phenanthroline-copper(I) complex [(OP)2Cu+] and hydrogen peroxide. This reaction specificity has been attributed to the creation of a binding site(s) for redox-active tetrahedral (OP)2Cu+ when RNA polymerase form productive complexes with promoters. This proposal has been confirmed for the Escherichia coli lac UV-5 promoter by the demonstration that the 2:1 2,9-dimethyl-1,10-phenanthroline-copper(I) complex [(Me2OP)2Cu+], a redox-inactive isostere of (OP)2-Cu+, protects the transcription start site from scission by the chemical nuclease activity. (Me2OP)2Cu+ is also an effective inhibitor of transcription. The inhibition of transcription and the protection from scission of the open complex by (OP)2Cu+ exhibit the same dependence on the concentration of (Me2OP)2Cu+. This redox- and exchange-stable species is a previously undescribed transcription inhibitor that binds to a site generated by the interaction of RNA polymerase with the promoter. Unlike the intercalating agent proflavine, which is also an effective transcription inhibitor, it does not displace the enzyme from the promoter. The ability of (Me2OP)2Cu+ to inhibit transcription may be partially responsible for its potent cytotoxicity.
1,10-菲咯啉-铜离子的核酸酶活性的致突变性。
DOI：
10.1016/s0006-291x(88)81090-8
发表时间：
1988
影响因子：
3.1
作者：
Feig,AL;Thederahn,T;Sigman,DS
通讯作者：
Sigman,DS