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[2,1-c][1,4]苯并二氮杂卓(PBD)-双缩放线菌素杂交体抑制DNA与转录因子Sp1的结合。

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

作者信息

Baraldi P G, Cacciari B, Guiotto A, Romagnoli R, Spalluto G, Leoni A, Bianchi N, Feriotto G, Rutigliano C, Mischiati C, Gambari R

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2000 Aug;19(8):1219-29. doi: 10.1080/15257770008033045.

DOI:10.1080/15257770008033045
PMID:11097052
Abstract

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 Sp1 were studied. The results obtained demonstrate that PBD-distamycin hybrid is a powerful inhibitor of Sp1/DNA interactions.

摘要

我们设计并合成了杂合物6,它是由与天然存在的氨茴霉素(2)和DC - 81(3)相关的小沟结合剂放线菌素A和吡咯并[2,1 - c][1,4]苯并二氮杂䓬(PBD)4组合而成。本文研究了化合物6对DNA与转录因子Sp1之间分子相互作用的影响。所得结果表明,PBD - 放线菌素杂合物是Sp1/DNA相互作用的强效抑制剂。

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[2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid inhibits DNA binding to transcription factor Sp1.[2,1-c][1,4]苯并二氮杂卓(PBD)-双缩放线菌素杂交体抑制DNA与转录因子Sp1的结合。
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Angew Chem Int Ed Engl. 2017 Jan 9;56(2):462-488. doi: 10.1002/anie.201510610. Epub 2016 Nov 15.
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Biosynthesis, synthesis, and biological activities of pyrrolobenzodiazepines.吡咯并苯二氮䓬类的生物合成、合成和生物活性。
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