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Curr Opin Drug Discov Devel. 2003 Sep;6(5):720-8.

Targeting I kappa B kinase for the treatment of inflammatory and other disorders.

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Bristol-Myers Squibb Pharmaceutical Research Institute, Immunology, Inflammation and Pulmonary Drug Discovery, PO Box 4000, Route 206 & Provinceline Road, Princeton, NJ 08543, USA.


The nuclear transcription factor NF kappa B plays a critical role in the pathogenesis of a number of human disorders, particularly those with an inflammatory component. Due to the fact that I kappa B kinase (IKK)-catalyzed phosphorylation of I kappa B proteins is an essential step in the signal-induced activation of NF kappa B, targeting this kinase represents a fascinating opportunity to develop novel therapeutics. In this review, the current understanding of the role of IKK/NF kappa B in disease processes will be discussed, along with evidence demonstrating that IKK inhibitors will be efficacious in disorders ranging from rheumatoid arthritis to cancer and diabetes. Potential mechanism-based toxicities will also be discussed.

[Indexed for MEDLINE]

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