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Inhibition of the DNA‐binding activity of NF‐κB by gold compounds in vitro

机译:体外金化合物对NF-κBDNA结合活性的抑制作用

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>Nuclear factor κB (NF-κB) is a transcription factor that is critical for the inducible expression of multiple cellular and viral genes. DNA binding activity is essential for its function. Here, we report that gold compounds, especially aurothioglucose (AuTG), have a strong inhibitory effect on NF-κB-DNA binding. Our finding also reveals that Zn2+ is a necessary component of NF-κB for its DNA binding activity and that gold ion can efficiently block NF-κB-DNA binding, presumably through oxidation of the cysteins associated with zinc. This redox mechanism may provide an explanation for the observed efficacy of gold compounds in the treatment of rheumatoid arthritis.
机译:p核因子κB(NF-κB)是一种转录因子,对于多种细胞和病毒基因的诱导表达至关重要。 DNA结合活性对其功能至关重要。在这里,我们报道了金化合物,特别是金硫葡糖(AuTG)对NF-κB-DNA结合具有很强的抑制作用。我们的发现还揭示了Zn 2 + 是NF-κB的DNA结合活性的必要成分,并且金离子可以有效地阻断NF-κB-DNA的结合,大概是通过与锌。这种氧化还原机制可以解释金化合物在类风湿关节炎治疗中观察到的功效。

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