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拓扑异构酶 II 和依托泊苷——一个纠结的故事。

Topoisomerase II and etoposide - a tangled tale.

机构信息

Cornell University, Ithaca NY, USA

出版信息

Nat Chem Biol. 2023 May;19(5):546-547. doi: 10.1038/s41589-022-01236-8.

DOI:10.1038/s41589-022-01236-8
PMID:36717712
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10159999/
Abstract

Etoposide, a chemotherapeutic poison of type IIA eukaryotic topoisomerases, promotes topoisomerase II to compact DNA by trapping DNA loops, creates DNA double-strand breaks, causes topo II to resist relocation, and pauses topisomerases’ ability to relax DNA supecoiling. Through these mechanisms, etoposide converts topoisomerase II into a roadblock to DNA processing.

摘要

依托泊苷是一种 IIA 型真核拓扑异构酶的化疗毒物,通过捕获 DNA 环促进拓扑异构酶 II 使 DNA 变紧密,造成 DNA 双链断裂,导致拓扑异构酶 II 抵抗重定位,并使拓扑异构酶的松弛 DNA 超螺旋的能力暂时停止。通过这些机制,依托泊苷将拓扑异构酶 II 转化为 DNA 加工的障碍。

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