PKIB Human

IKK-β is a component of the IκB kinase (IKK) complex, which is involved in the activation of the transcription factor NF-κB (Nuclear Factor kappa-light-chain-enhancer of activated B cells) . The activation of NF-κB is a key step in the immune response, as it controls the expression of various genes involved in inflammation, immune response, cell proliferation, and survival .

When activated, IKK-β phosphorylates the inhibitor of NF-κB, known as IκB. This phosphorylation marks IκB for degradation via the ubiquitination pathway, thereby freeing NF-κB to enter the nucleus and activate target genes .

IKK-β has been implicated in various diseases, particularly those involving inflammation and immune dysregulation. For instance, it plays a significant role in brain cells following a stroke. Blocking NF-κB activation by IKK-β can help damaged brain cells survive and potentially recover .

Moreover, the inhibition of IKK-β and related kinases has been explored as a therapeutic strategy for treating inflammatory diseases and cancer . For example, the small-molecule inhibitor SAR113945, developed by Sanofi-Aventis, was evaluated in patients with knee osteoarthritis .

Protein kinase inhibitors, including those targeting IKK-β, have become significant drug targets for various conditions. Historically, these inhibitors have been used to treat cancer, cardiovascular diseases, autoimmune, and inflammatory processes . The development of peptide-based inhibitors has also emerged as a promising approach due to their ability to mimic specific substrate-interaction domains of protein kinases .