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

被引:21
作者
Baraldi, PG [1 ]
Cacciari, B
Guiotto, A
Romagnoli, R
Spalluto, G
Leoni, A
Bianchi, N
Feriotto, G
Rutigliano, C
Mischiati, C
Gambari, R
机构
[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy
[2] Univ Ferrara, Dipartmento Biochim & Biol Mol, I-44100 Ferrara, Italy
关键词
D O I
10.1080/15257770008033045
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
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收藏
页码:1219 / 1229
页数:11
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