3.8 Article

A nuclear factor-κB inhibitor BAY 11-7082 suppresses endothelin-1 production in cultured vascular endothelial cells

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JAPANESE JOURNAL OF PHARMACOLOGY
卷 89, 期 1, 页码 81-84

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JAPANESE PHARMACOLOGICAL SOC
DOI: 10.1254/jjp.89.81

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nuclear factor-kappa B; endothelin-1; tumor necrosis factor-alpha

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BAY 11-7082, an inhibitor of nuclear factor-kappaB (NF-kappaB), which prevents a step of the phosphorylation of inhibitory protein IkappaB bound to NF-kappaB, suppressed basal and tumor necrosis factor (TNF)-alpha-induced prepro endothelin (ET)-1 mRNA expression and NF-kappaB activation in cultured vascular endothelial cells. BAY 11-7082 significantly decreased basal and TNF-alpha-induced ET-1 release from endothelial cells. These results indicate that the inhibition of NF-kappaB activation contributes to the suppressive effect of BAY 11-7082 on ET-1 gene expression and ET-1 release, thereby suggesting that NF-kappaB plays an important role in the regulation of ET-1 production.

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