Inhibitors of κB Kinase (IKK) and Nuclear Factor Kappa-B (NF-κB): Attractive Drug Targets

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 20 July 2024 | Viewed by 133

Special Issue Editor


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Guest Editor
Department of Molecular and Structural Biochemistry, North Carolina State University, Raleigh, NC 27695, USA
Interests: IκB kinase; small molecule kinase inhibitors; peptide inhibitors

Special Issue Information

The dysregulation of IKK/NF-kB has been shown to be associated with inflammatory and autoimmune diseases, given the fact that the IKK/NF-kB pathways play a central role in immune and inflammatory responses. In addition, IKK/NF-kB-mediated inflammation is essential for the pathogenesis of other common human diseases such as cancer, diabetes, cardiac dysfunction and aging. In the past decade, the growing interest in targeting IKK to attenuate NF-kB activities under pathological conditions has resulted in the identification of many small molecule IKK kinase inhibitors for disease treatment, most of which are ATP competitive kinase inhibitors. However, using these high-affinity small-molecule kinase inhibitors has often resulted in severe side effects such as septic shock due to elevated IL-1b secretion and TNF-dependent T and B cell depletion. Interestingly, applying peptides to inhibit NEMO-IKKb interaction has shown the beneficial effects of down-regulating IKK/NF-kB activity while exhibiting limited side effects.

Since the direct pharmacologic inhibition of IKKb kinase activity has limited value in disease treatment, targeting NEMO-IKKb interaction or other protein–protein interaction interfaces to attenuate excessive IKKb activation under pathological conditions is considered as a promising strategy to develop novel therapeutics. In this special Issue, we invite authors in this field to report their original research discoveries pertaining to novel therapeutic approaches for targeting IKK. We are especially interested in novel research strategies that target allosteric sites and other protein–protein interaction interfaces, thereby inhibiting IKK activation, which would avoid severe side effects due to induced apoptosis and IL-1b secretion.

Dr. Guozhou Xu
Guest Editor

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Keywords

  • IkB kinase
  • kinase activation
  • protein–protein interaction
  • ATP-competitive small-molecule kinase inhibitor
  • inflammatory disease
  • autoimmune disease

Published Papers

This special issue is now open for submission.
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