TRIPLE HELIX SPECIFIC LIGANDS
TRIPLE HELIX SPECIFIC LIGANDS
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DOI：
10.1126/science.256.5064.1681
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发表时间：
1992-06-19
期刊：
影响因子：
56.9
通讯作者：
HELENE, C
中科院分区：
文献类型：
--
作者：
MERGNY, JL;DUVALVALENTIN, G;HELENE, C
寡脱氧核苷酸与双链 DNA 的大沟结合后形成三螺旋。苯并[e]吡啶并吲哚衍生物 (BePI) 强烈稳定了该结构，并显示出优先与三链体而不是双链体结合。能量转移实验表明 BePI 嵌入三螺旋内。当 BePI 稳定三链体时，形成三链体的寡脱氧核苷酸对大肠杆菌 RNA 聚合酶对特定基因转录起始的序列特异性抑制会大大增强。在紫外线照射下，BePI 会诱导三螺旋结构内靶标的共价修饰。
A triple helix is formed upon binding of an oligodeoxynucleotide to the major groove of duplex DNA. A benzo[e]pyridoindole derivative (BePI) strongly stabilized this structure and showed preferential binding to a triplex rather than to a duplex. Energy transfer experiments suggest that BePI intercalates within the triple helix. Sequence-specific inhibition of transcription initiation of a specific gene by Escherichia coli RNA polymerase by a triplex-forming oligodeoxynucleotide is strongly enhanced when the triplex is stabilized by BePI. Upon irradiation with ultraviolet light, BePI induces covalent modifications of the target within the triple helix structure.