Title: Study of the inhibitory effects on <scp>TNF</scp>‐α‐induced <scp>NF</scp>‐κB activation of <scp>IMD</scp>0354 analogs
Abstract:Nuclear factor–κB ( NF –κB) is an important nuclear transcription factor which regulates pro‐inflammatory cytokines such as TNF ‐α, IL ‐6. Its role as immunoregulatory mediator makes it an attractive ...Nuclear factor–κB ( NF –κB) is an important nuclear transcription factor which regulates pro‐inflammatory cytokines such as TNF ‐α, IL ‐6. Its role as immunoregulatory mediator makes it an attractive target in the development of treatments for inflammatory and autoimmune diseases. In this study, we synthesized derivatives of IMD 0354, a known inhibitor for NF ‐κB, in attempt to understand the effect of benzanilide substitutions on its activity. The inhibition of these analogs on NF ‐κB activation was analyzed by luciferase assay. The inhibition of IKK β phosphorylation and pro‐inflammatory cytokines was determined by Western blot and real‐time PCR . The structure activity relationships showed that the hydroxyl group on IMD 0354 is a critical moiety that resulting in the inhibition of NF ‐κB. Derivatives 1m , 2b, and 2c were shown to inhibit pro‐inflammatory cytokine production at low concentration. These newly synthesized compounds may be useful for the treatment of chronic inflammatory disorders or for cancer prevention.Read More
Publication Year: 2017
Publication Date: 2017-05-30
Language: en
Type: letter
Indexed In: ['crossref', 'pubmed']
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Cited By Count: 8
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Title: $Study of the inhibitory effects on <scp>TNF</scp>‐α‐induced <scp>NF</scp>‐κB activation of <scp>IMD</scp>0354 analogs
Abstract: Nuclear factor–κB ( NF –κB) is an important nuclear transcription factor which regulates pro‐inflammatory cytokines such as TNF ‐α, IL ‐6. Its role as immunoregulatory mediator makes it an attractive target in the development of treatments for inflammatory and autoimmune diseases. In this study, we synthesized derivatives of IMD 0354, a known inhibitor for NF ‐κB, in attempt to understand the effect of benzanilide substitutions on its activity. The inhibition of these analogs on NF ‐κB activation was analyzed by luciferase assay. The inhibition of IKK β phosphorylation and pro‐inflammatory cytokines was determined by Western blot and real‐time PCR . The structure activity relationships showed that the hydroxyl group on IMD 0354 is a critical moiety that resulting in the inhibition of NF ‐κB. Derivatives 1m , 2b, and 2c were shown to inhibit pro‐inflammatory cytokine production at low concentration. These newly synthesized compounds may be useful for the treatment of chronic inflammatory disorders or for cancer prevention.