AI Article Synopsis
- Aurintricarboxylic acid (ATA) is recognized as a strong inhibitor of NF-kappaB's ability to bind DNA, and this study explores the effectiveness of its analogues.
- Among the analogues, bromopyrogallol red (BPR) emerged as the most potent inhibitor of NF-kappaB-DNA binding, creating strong hydrogen bonds with the p50 subunit of NF-kappaB.
- Additionally, BPR forms a stable complex with zinc, which is known to influence NF-kappaB's DNA binding, and it has been identified as the most effective antioxidant in this group of analogues.
Article Abstract
Previously, we have reported that aurintricarboxylic acid (ATA) is one of the most potent inhibitors of the DNA binding of transcription factor NF-kappaB. We now report the NF-kappaB-DNA binding inhibitory activity of ATA analogues. An electrophoretic mobility shift assay has shown that bromopyrogallol red (BPR) is the most effective inhibitor of NF-kappaB-DNA binding among the studied analogues. The molecular modeling studies showed that BPR makes a strong network of hydrogen bonds with the DNA-binding region of the p50 subunit of NF-kappaB and has electronegative potential on its peripheral surface. Because zinc has been reported to influence the DNA binding of NF-kappaB, the interaction of these analogues with zinc was studied. Chemical speciation and formation-constant studies showed that BPR forms the most stable 1:1 complex with zinc. BPR has also been found to be the most potent antioxidant among the studied analogues.
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