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Mediators Inflamm. 2012;2012:416036. doi: 10.1155/2012/416036. Epub 2012 Jun 15.

BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets.

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1
College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.

Abstract

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 E(2), 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.

PMID:
22745523
PMCID:
PMC3382285
DOI:
10.1155/2012/416036
[Indexed for MEDLINE]
Free PMC Article
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