Abstract
The IκB kinases (IKKs) are essential components of the signaling pathway by which the NF-κB p50/RelA transcription factor is activated in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS) and tumor necrosis factor (TNFα). NF-κB signaling results in the expression of numerous genes involved in innate and adaptive immune responses. The pathway is also implicated in chronic inflammatory disorders including rheumatoid arthritis (RA), chronic obstructive pulmonary disorder (COPD), and asthma. Inhibition of the kinase activity of the IKKs is therefore a promising mechanism for intervention in these diseases. Here, we will review the literature describing small molecule inhibitors of IKKβ (IKK2), the most widely studied of the IKKs.
Keywords: I-kappa B kinase inhibitors, IKK, IKKβ, NF-κB, inflammation
Current Topics in Medicinal Chemistry
Title: Progress Towards the Development of Anti-Inflammatory Inhibitors of IKKβ
Volume: 9 Issue: 7
Author(s): Paul Bamborough, James F. Callahan, John A. Christopher, Jeffrey K. Kerns, John Liddle, David D. Miller, Mary A. Morse, William L. Rumsey and Rick Williamson
Affiliation:
Keywords: I-kappa B kinase inhibitors, IKK, IKKβ, NF-κB, inflammation
Abstract: The IκB kinases (IKKs) are essential components of the signaling pathway by which the NF-κB p50/RelA transcription factor is activated in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS) and tumor necrosis factor (TNFα). NF-κB signaling results in the expression of numerous genes involved in innate and adaptive immune responses. The pathway is also implicated in chronic inflammatory disorders including rheumatoid arthritis (RA), chronic obstructive pulmonary disorder (COPD), and asthma. Inhibition of the kinase activity of the IKKs is therefore a promising mechanism for intervention in these diseases. Here, we will review the literature describing small molecule inhibitors of IKKβ (IKK2), the most widely studied of the IKKs.
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Cite this article as:
Bamborough Paul, Callahan F. James, Christopher A. John, Kerns K. Jeffrey, Liddle John, Miller D. David, Morse A. Mary, Rumsey L. William and Williamson Rick, Progress Towards the Development of Anti-Inflammatory Inhibitors of IKKβ, Current Topics in Medicinal Chemistry 2009; 9 (7) . https://dx.doi.org/10.2174/156802609789007336
DOI https://dx.doi.org/10.2174/156802609789007336 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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