Champoux J J
Department of Microbiology, Box 357242, University of Washington, Seattle, Washington 98195-7242, USA.
Ann N Y Acad Sci. 2000;922:56-64. doi: 10.1111/j.1749-6632.2000.tb07025.x.
The sole target for the anticancer drug camptothecin (CPT) is the type I topoisomerase. The drug poisons the topoisomerase by slowing the religation step of the reaction, thereby trapping the enzyme in a covalent complex on the DNA. In addition, CPT has been shown to inhibit plasmid DNA relaxation in vitro. The structural bases for these two activities of CPT are explored in relation to the recently published crystal structure of the enzyme with bound DNA.
抗癌药物喜树碱（CPT）的唯一靶点是I型拓扑异构酶。该药物通过减缓反应的重新连接步骤来毒害拓扑异构酶，从而将酶捕获在DNA上的共价复合物中。此外，CPT已被证明在体外可抑制质粒DNA松弛。结合最近发表的该酶与结合DNA的晶体结构，探讨了CPT这两种活性的结构基础。
Zotero 插件