Abstract
During the last two decades, the studies on ubiquitination in regulating transcription factor NF-κB activation have elucidated the expanding role of ubiquitination in modulating cellular events by non-proteolytic mechanisms, as well as by proteasomal degradation. The significance of ubiquitination has also been recognized in regulating gene transcription, epigenetic modifications, kinase activation, DNA repair and subcellular translocation. This progress has been translated into novel strategies for developing anti-cancer therapeutics, exemplified by the success of the first FDA-approved proteasome inhibitor drug Bortezomib. Here we discuss the current understanding of the ubiquitin-proteasome system and how it is involved in regulating NF-κB signaling pathways in response to a variety of stimuli. We also focus on the recent progress of anti-cancer drug development targeting various steps of ubiquitination process, and the potential of these drugs in cancer treatment as related to their impact on NF-κB activation.
Keywords: Ubiquitin, NF-κB, cancer, therapeutics.
Current Pharmaceutical Design
Title:When Ubiquitin Meets NF-κB: A Trove for Anti-cancer Drug Development
Volume: 19 Issue: 18
Author(s): Zhao-Hui Wu and Yuling Shi
Affiliation:
Keywords: Ubiquitin, NF-κB, cancer, therapeutics.
Abstract: During the last two decades, the studies on ubiquitination in regulating transcription factor NF-κB activation have elucidated the expanding role of ubiquitination in modulating cellular events by non-proteolytic mechanisms, as well as by proteasomal degradation. The significance of ubiquitination has also been recognized in regulating gene transcription, epigenetic modifications, kinase activation, DNA repair and subcellular translocation. This progress has been translated into novel strategies for developing anti-cancer therapeutics, exemplified by the success of the first FDA-approved proteasome inhibitor drug Bortezomib. Here we discuss the current understanding of the ubiquitin-proteasome system and how it is involved in regulating NF-κB signaling pathways in response to a variety of stimuli. We also focus on the recent progress of anti-cancer drug development targeting various steps of ubiquitination process, and the potential of these drugs in cancer treatment as related to their impact on NF-κB activation.
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Cite this article as:
Wu Zhao-Hui and Shi Yuling, When Ubiquitin Meets NF-κB: A Trove for Anti-cancer Drug Development, Current Pharmaceutical Design 2013; 19 (18) . https://dx.doi.org/10.2174/1381612811319180010
DOI https://dx.doi.org/10.2174/1381612811319180010 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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