Sequence-specific trapping of topoisomerase I by DNA binding polyamide-camptothecin conjugates.
Sequence-specific trapping of topoisomerase I by DNA binding polyamide-camptothecin conjugates.
复制标题
通过 DNA 结合聚酰胺-喜树碱缀合物对拓扑异构酶 I 进行序列特异性捕获。
DOI：
10.1021/ja010392p
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发表时间：
2001
影响因子：
15
通讯作者：
Dervan,PB
中科院分区：
文献类型：
--
作者：
Wang,CC;Dervan,PB
Hairpin pyrrole−imidazole polyamides are synthetic ligands that bind in the minor groove of DNA with affinities and specificities comparable to those of DNA binding proteins. Three polyamide−camptothecin conjugates1−3with linkers varying in length between 7, 13, and 18 atoms were synthesized to trap the enzyme Topoisomerase I and induce cleavage at predetermined DNA sites. One of these, polyamide−camptothecin conjugate3at nanomolar concentration (50 nM) in the presence of Topo I (37 °C), induces DNA cleavage between three and four base pairs from the polyamide binding site in high yield (77%).
