Programmable oligomers targeting 5′-GGGG-3′ in the minor groove of DNA and NF-κB binding inhibition

被引:19
作者
Chenoweth, David M. [1 ]
Poposki, Julie A. [1 ]
Marques, Michael A. [1 ]
Dervan, Peter B. [1 ]
机构
[1] CALTECH, Div Chem & Chem Engn, Pasadena, CA 91125 USA
关键词
D O I
10.1016/j.bmc.2006.10.051
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
A series of hairpin oligomers containing benzimidazole (Bi) and imidazopyridine (I) rings were synthesized and screened to target 5'-WGGGGW-3', a core sequence in the DNA-binding site of NF-kappa B, a prolific transcription factor important in biology and disease. Five Bi and Ip containing oligomers bound to the 5'-WGGGGW-3' site with high affinity. One of the oligomers (Im-Im-Im-Im-gamma-Py-Bi-Py-Bi-beta-Dp) was able to inhibit DNA binding by the transcription factor NF-kappa B, (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:759 / 770
页数:12
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