Piestrzeniewicz M, Studzian K, Wilmańska D, Płucienniczak G, Gniazdowski M
Department of General Chemistry, Institute of Physiology and Biochemistry, Medical University in Lódz, Poland.
Acta Biochim Pol. 1998;45(1):127-32.
9-Aminoacridine carboxamide derivatives studied here form with DNA intercalative complexes which differ in the kinetics of dissociation. Inhibition of total RNA synthesis catalyzed by phage T7 and Escherichia coli DNA-dependent RNA polymerases correlates with the formation of slowly dissociating acridine-DNA complex of time constant of 0.4-2.3 s. Their effect on RNA synthesis is compared with other ligands which form with DNA stable complexes of different steric properties. T7 RNA polymerase is more sensitive to distamycin A and netropsin than the E. coli enzyme while less sensitive to actinomycin D. Actinomycin induces terminations in the transcript synthesized by T7 RNA polymerase. Despite low dissociation rates of DNA complexes with acridines and pyrrole antibiotics no drug dependent terminations are observed with these ligands.
本文所研究的9-氨基吖啶羧酰胺衍生物与DNA形成了解离动力学不同的嵌入复合物。噬菌体T7和大肠杆菌DNA依赖性RNA聚合酶催化的总RNA合成的抑制作用与时间常数为0.4 - 2.3秒的缓慢解离的吖啶-DNA复合物的形成相关。将它们对RNA合成的影响与其他与DNA形成具有不同空间性质的稳定复合物的配体进行了比较。T7 RNA聚合酶比大肠杆菌酶对偏端霉素A和纺锤菌素更敏感，而对放线菌素D较不敏感。放线菌素会诱导T7 RNA聚合酶合成的转录本发生终止。尽管吖啶和吡咯类抗生素与DNA复合物的解离速率较低，但这些配体未观察到药物依赖性终止。
