Small molecule inhibitors of IKK kinase activity

Abstract

The nuclear transcription factor NF-κB plays a significant role in the pathogenesis of a variety of diseases. Because of the key role played by the inhibitor of κB kinase (IKK) complex in the activation of NF-κB, coupled with the druggability of kinases as a target class, numerous companies have been pursuing discovery programmes aimed at identifying small molecule inhibitors of these enzymes. This paper reviews the patenting activity associated with these efforts.

Keywords::

• cancer
• IκB
• IKK-1
• IKK-2
• IKK-3
• inflammation
• NF-κB

Acknowledgement

The authors would like to thank L Anderson of Bayer’s Scientific Library for his extensive help in identifying and obtaining the literature sources on which this article is based.