[2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid inhibits DNA binding to transcription factor Sp1

[2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid inhibits DNA binding to transcription factor Sp1
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DOI:
10.1080/15257770008033045
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发表时间:
2000-01-01
影响因子:
1.3
通讯作者:
Gambari, R
Gambari, R
中科院分区:
生物学4区
文献类型:
--
作者:
Baraldi, PG;Cacciari, B;Gambari, R

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我们设计并合成了杂合物6,将小沟结合剂偏端霉素A和吡咯并[2,1-c][1,4]苯并二氮杂卓(PBD)4结合制备,与天然存在的安曲霉素(2)和DC-81(3)相关。本文研究了化合物6对DNA与转录因子Spl分子相互作用的影响。结果表明,PBD-偏端霉素杂合物是Sp1/DNA相互作用的强抑制剂。
We designed and synthesized the hybrid 6, prepared combining the minor groove binders distamycin A and pyrrolo [2,1-c][1,4] benzodiazepine (PBD) 4, related to the natural occurring anthramycin (2) and DC-81 (3). In this paper, the effects of the compound 6 on molecular interactions between DNA and transcription factor Spl were studied. The results obtained demonstrate that PBD-distamycin hybrid is a powerful inhibitor of Sp1/DNA interactions.