Open AccessA Nuclear Factor-κdB Inhibitor BAY 11-7082 Suppresses Endothelin-1 Production in Cultured Vascular Endothelial Cells
Author(s) -
Mamoru Ohkita,
Masanori Takaoka,
Yasuko Shiota,
Rumi Nojiri,
Masato Sugii,
Yasuo Matsumura
Publication year - 2002
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - Uncategorized
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.89.81
Subject(s) - endothelin 1 , tumor necrosis factor alpha , nf κb , endothelin receptor , basal (medicine) , medicine , phosphorylation , endocrinology , microbiology and biotechnology , nfkb1 , biology , chemistry , signal transduction , transcription factor , gene , biochemistry , receptor , insulin
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.