Tsao Y P, Russo A, Nyamuswa G, Silber R, Liu L F
Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School, Piscataway 08854.
Cancer Res. 1993 Dec 15;53(24):5908-14.
The extreme S-phase-specific cytotoxicity of camptothecin has been shown to involve active DNA replication. To investigate the role of DNA replication in camptothecin cytotoxicity, we have studied the interaction between the DNA replication machinery and the topoisomerase I-camptothecin-DNA ternary cleavable complex in a cell-free SV40 DNA replication system. The formation of topoisomerase I-camptothecin-DNA-cleavable complexes on the replication template efficiently and irreversibly inhibited DNA replication. Two aberrant forms of replication products were produced whose abundance varied with the concentrations of exogenously added topoisomerase I and camptothecin. At low concentrations of topoisomerase I and camptothecin, the major aberrant DNA replication product was close-to-unit-length-linear DNA, while at higher concentrations the predominant product was close-to-dimer-size-linear DNA. Analysis of these aberrant replication products has suggested a "collision" model in which the interaction between an advancing replication fork and a topoisomerase I-camptothecin-DNA-cleavable complex results in irreversible arrest of the replication fork and the formation of a double-strand DNA break at the fork. Concomitant with fork arrest and fork breakage, the reversible cleavable complex was converted into a topoisomerase I-linked DNA break. We propose that one or several of these events triggers S-phase-specific cell killing and G2-phase cell cycle arrest.
喜树碱具有极强的S期特异性细胞毒性,这已被证明与活跃的DNA复制有关。为了研究DNA复制在喜树碱细胞毒性中的作用,我们在无细胞的SV40 DNA复制系统中研究了DNA复制机制与拓扑异构酶I - 喜树碱 - DNA三元可裂解复合物之间的相互作用。复制模板上拓扑异构酶I - 喜树碱 - DNA可裂解复合物的形成有效且不可逆地抑制了DNA复制。产生了两种异常形式的复制产物,其丰度随外源添加的拓扑异构酶I和喜树碱的浓度而变化。在低浓度的拓扑异构酶I和喜树碱下,主要的异常DNA复制产物是接近单位长度的线性DNA,而在较高浓度下,主要产物是接近二聚体大小的线性DNA。对这些异常复制产物的分析提出了一种“碰撞”模型,其中前进的复制叉与拓扑异构酶I - 喜树碱 - DNA可裂解复合物之间的相互作用导致复制叉的不可逆停滞以及在叉处形成双链DNA断裂。伴随着叉的停滞和叉的断裂,可逆的可裂解复合物转化为拓扑异构酶I连接的DNA断裂。我们提出这些事件中的一个或几个触发了S期特异性细胞杀伤和G2期细胞周期停滞。