AI Article Synopsis
- IKK-beta is an important protein kinase that activates the transcription factor NF-kappaB during inflammation.
- Researchers discovered a small molecule that inhibits IKK-beta and improved its potency through optimization.
- The refined inhibitors showed strong effectiveness in reducing cytokine release in a specific inflammatory model using LPS.
Article Abstract
IkappaB kinase beta (IKK-beta) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-kappaB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-beta. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-beta inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFalpha).
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| http://dx.doi.org/10.1016/s0960-894x(02)01046-6 | DOI Listing |
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