Garg L C, DiAngelo S, Jacob S T
Proc Natl Acad Sci U S A. 1987 May;84(10):3185-8. doi: 10.1073/pnas.84.10.3185.
The fraction DE-B obtained by fractionating an extract from rat mammary adenocarcinoma cells on a DEAE-Sephadex column was used for transcribing linear and supercoiled rRNA gene (rDNA). This fraction, which is known to contain RNA polymerase I and essential transcription factors, also contains DNA topoisomerase I activity. Inhibition of this topoisomerase activity by the selective inhibitor camptothecin markedly diminished transcription of supercoiled rDNA, and at a concentration of 150 microM, camptothecin almost completely inhibited DNA topoisomerase I activity and supercoiled rDNA transcription. Addition of exogenous calf thymus DNA topoisomerase I to the sample containing the drug restored the ability of the extract to transcribe supercoiled rDNA. Camptothecin, even at a concentration of 500 microM, had no significant effect on the transcription of linear rDNA. These studies show that relaxation of supercoiled rDNA by DNA topoisomerase I is essential for its transcription. The preferential inhibition of rRNA synthesis in vivo following treatment with camptothecin is probably due to selective camptothecin inhibition of DNA topoisomerase I activity.
通过在DEAE - 葡聚糖凝胶柱上对大鼠乳腺腺癌细胞提取物进行分级分离得到的DE - B级分,用于转录线性和超螺旋rRNA基因(rDNA)。该级分已知含有RNA聚合酶I和必需的转录因子,还具有DNA拓扑异构酶I活性。选择性抑制剂喜树碱对这种拓扑异构酶活性的抑制显著降低了超螺旋rDNA的转录,在150微摩尔浓度下,喜树碱几乎完全抑制了DNA拓扑异构酶I活性和超螺旋rDNA转录。向含药样品中添加外源小牛胸腺DNA拓扑异构酶I可恢复提取物转录超螺旋rDNA的能力。即使在500微摩尔浓度下,喜树碱对线性rDNA的转录也没有显著影响。这些研究表明,DNA拓扑异构酶I介导的超螺旋rDNA松弛对其转录至关重要。喜树碱处理后体内rRNA合成的优先抑制可能是由于喜树碱对DNA拓扑异构酶I活性的选择性抑制。