[HTML][HTML] Molecular design and biological activities of NF-κB inhibitors
K Umezawa, C Chaicharoenpong - Molecules and cells, 2002 - Elsevier
NF-κB is a transcription factor that induces inflammatory cytokines and anti-apoptotic
proteins. We designed a new NF-κB inhibitor that is based on the structure of the antibiotic
epoxyquinomicin C. The designed compound, dehydroxymethyl-epoxyquino-micin
(DHMEQ), inhibited the TNF-α-induced activation of NF-κB, and showed an anti-arthritic
effect in mice. Recently, we looked into its mechanism of inhibition. DHMEQ inhibited the
TNF-α-induced cellular DNA binding of nuclear NF-κB, but not the phosphorylation or …
proteins. We designed a new NF-κB inhibitor that is based on the structure of the antibiotic
epoxyquinomicin C. The designed compound, dehydroxymethyl-epoxyquino-micin
(DHMEQ), inhibited the TNF-α-induced activation of NF-κB, and showed an anti-arthritic
effect in mice. Recently, we looked into its mechanism of inhibition. DHMEQ inhibited the
TNF-α-induced cellular DNA binding of nuclear NF-κB, but not the phosphorylation or …