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首页> 外文期刊>Life sciences >Role of cysteine residues of p65/NF-kappaB on the inhibition by the sesquiterpene lactone parthenolide and N-ethyl maleimide, and on its transactivating potential.
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Role of cysteine residues of p65/NF-kappaB on the inhibition by the sesquiterpene lactone parthenolide and N-ethyl maleimide, and on its transactivating potential.

机译：p65 /NF-κB的半胱氨酸残基在倍半萜内酯单酚和N-乙基马来酰亚胺的抑制作用及其反式激活潜力中的作用。

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摘要

Sesquiterpene lactones (SLs) are potent anti-inflammatory substances. It was previously shown that the anti-inflammatory effect could be partly explained by the inhibition of the transcription factor NF-kappaB. Whether they inhibit the DNA binding of NF-kappaB, the activation of the IkappaB-kinase, or both is still a matter of debate. The data supporting these hypotheses were obtained using different cell systems. In this contribution we analyzed the mechanism of the sesquiterpene lactone-mediated inhibition using different cell systems, and showed that in all the cell lines analyzed, SLs inhibited both NF-kappaB binding and the IkappaB-kinase, but that the former played a more preponderant role in the inhibition. These results again confirm the importance of cysteine 38 in the inhibition and regulation of NF-kappaB's function. Moreover, we compared the selectivity of the SL parthenolide with that of N-ethyl maleimide (NEM). We showed that NEM directly alkylated p65 as well as p50 of NF-kappaB, whereasSLs possess a selectivity towards p65. Finally, we studied the transactivating properties of various p65 mutants, to analyze the effect of exchanged cysteine residues in the DNA binding domain of NF-kappaB/p65 on its function and demonstrated that the transactivating potential of the mutants did not correlate with their DNA binding strenght.
机译：倍半萜内酯（SLs）是有效的抗炎物质。先前显示抗炎作用可以部分地通过抑制转录因子NF-κB来解释。它们是否抑制NF-κB的DNA结合，IkappaB激酶的激活或两者均仍是一个争论的问题。使用不同的细胞系统获得支持这些假设的数据。在这项研究中，我们使用不同的细胞系统分析了倍半萜内酯介导的抑制作用的机制，并表明在所有分析的细胞系中，SL均抑制NF-κB结合和IkappA-激酶，但前者发挥了更大的作用。有抑制作用。这些结果再次证实了半胱氨酸38在抑制和调节NF-κB功能中的重要性。此外，我们比较了SL苯酚和N-乙基马来酰亚胺（NEM）的选择性。我们表明，NEM直接将p65以及NF-κB的p50烷基化，而SLs对p65具有选择性。最后，我们研究了各种p65突变体的反式激活特性，以分析NF-kappaB / p65的DNA结合结构域中交换的半胱氨酸残基对其功能的影响，并证明了该突变体的反式激活潜力与其DNA结合无关实力。

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