Evans Blue is an inhibitor of nuclear factor-kappa B (NF-κB)-DNA binding
Evans Blue is an inhibitor of nuclear factor-kappa B (NF-κB)-DNA binding
复制标题
DOI：
10.1016/j.bmcl.2004.07.096
复制
发表时间：
2004-12-20
影响因子：
2.7
通讯作者：
Ramos, MJ
中科院分区：
文献类型：
--
作者：
Sharma, RK;Otsuka, M;Ramos, MJ
核因子κ B （NF-KB）是一种重要的转录因子，参与许多免疫和炎症反应。它在HIV-1长末端重复序列中具有kappa B结合位点，因此对HIV基因表达至关重要。因此，靶向NF-KB阻止其DNA结合具有重要的治疗潜力。在这种情况下，我们报道了Evans Blue作为NF-kappaB-DNA结合的新型抑制剂。Evans Blue在100 PM的低浓度下抑制NF-KB的DNA结合。此外，利用对接和产生静电电位图的分子建模研究预测了EB与NF-kappaB DNA结合区域的可能结合模式，与实验活性一致。(C) 2004 Elsevier Ltd.版权所有。
Nuclear factor-kappa B (NF-KB) is an important transcription factor, involved in many immune and inflammatory responses. It is critical in HIV gene expression as it has kappa B binding sites in the HIV-1 long-terminal repeat. Hence, targeting NF-KB to prevent its DNA binding holds a significant therapeutic potential. In this context, we report Evans Blue as a novel inhibitor of NF-kappaB-DNA binding. Evans Blue was found to be inhibiting DNA binding of NF-KB at a low concentration of 100 PM. Further, molecular modeling studies using docking and generation of electrostatic potential maps predicted a possible binding mode of EB to the DNA binding region of NF-kappaB, consistent with the experimental activity. (C) 2004 Elsevier Ltd. All rights reserved.