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BAY 11-7082 Is a Broad-Spectrum Inhibitor with Anti-Inflammatory Activity against Multiple Targets

Lee, Jaehwi ; Rhee, Man Hee ; Kim, Eunji ; Cho, Jae Youl Fantuzzi, Giamila

Mediators of Inflammation, 2012-01, Vol.2012, p.416036-11 [Periódico revisado por pares]

United States: Hindawi Limiteds

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Título:
BAY 11-7082 Is a Broad-Spectrum Inhibitor with Anti-Inflammatory Activity against Multiple Targets
Autor: Lee, Jaehwi ; Rhee, Man Hee ; Kim, Eunji ; Cho, Jae Youl
Fantuzzi, Giamila
Assuntos: Animals ; Anti-Inflammatory Agents - pharmacology ; Cell Line ; Cell Survival - drug effects ; Dinoprostone - genetics ; Dinoprostone - metabolism ; Humans ; Immunoblotting ; Male ; Mice ; Mice, Inbred C57BL ; NF-kappa B - genetics ; NF-kappa B - metabolism ; Nitric Oxide - metabolism ; Nitriles - pharmacology ; Sulfones - pharmacology ; Tumor Necrosis Factor-alpha - metabolism
É parte de: Mediators of Inflammation, 2012-01, Vol.2012, p.416036-11
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Academic Editor: Giamila Fantuzzi
Descrição: BAY 11-7082 (BAY) is an inhibitor of κB kinase (IKK) that has pharmacological activities that include anticancer, neuroprotective, and anti-inflammatory effects. In this study, BAY-pharmacological target pathways were further characterized to determine how this compound simultaneously suppresses various responses. Primary and cancerous (RAW264.7 cells) macrophages were activated by lipopolysaccharide, a ligand of toll-like receptor 4. As reported previously, BAY strongly suppressed the production of nitric oxide, prostaglandin E2, and tumor necrosis factor-α and reduced the translocation of p65, major subunit of nuclear factor-κB, and its upstream signaling events such as phosphorylation of IκBα, IKK, and Akt. In addition, BAY also suppressed the translocation and activation of activator protein-1, interferon regulatory factor-3, and signal transducer and activator of transcription-1 by inhibiting the phosphorylation or activation of extracellular signal-related kinase, p38, TANK-binding protein, and Janus kinase-2. These data strongly suggest that BAY is an inhibitor with multiple targets and could serve as a lead compound in developing strong anti-inflammatory drugs with multiple targets in inflammatory responses.
Editor: United States: Hindawi Limiteds
Idioma: Inglês

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BAY 11-7082 Is a Broad-Spectrum Inhibitor with Anti-Inflammatory Activity against Multiple Targets

Lee, Jaehwi ; Rhee, Man Hee ; Kim, Eunji ; Cho, Jae Youl Fantuzzi, Giamila

United States: Hindawi Limiteds

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