BAY 11-7082 Is a Broad-Spectrum Inhibitor with Anti-Inflammatory Activity against Multiple Targets
- Authors
- Lee, Jaehwi; Rhee, Man Hee; Kim, Eunji; Cho, Jae Youl
- Issue Date
- 2012
- Publisher
- HINDAWI PUBLISHING CORPORATION
- Citation
- MEDIATORS OF INFLAMMATION, v.2012
- Journal Title
- MEDIATORS OF INFLAMMATION
- Volume
- 2012
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/20968
- DOI
- 10.1155/2012/416036
- ISSN
- 0962-9351
1466-1861
- Abstract
- BAY 11-7082 (BAY) is an inhibitor of kappa B 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 E-2, and tumor necrosis factor-alpha and reduced the translocation of p65, major subunit of nuclear factor-kappa B, and its upstream signaling events such as phosphorylation of I kappa B alpha, 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.
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Collections - College of Pharmacy > School of Pharmacy > 1. Journal Articles
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