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Drug discovery today · May 2014
ReviewSmall molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases.
- Frank J Dekker, Thea van den Bosch, and Nathaniel I Martin.
- Pharmaceutical Gene Modulation, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: f.j.dekker@rug.nl.
- Drug Discov. Today. 2014 May 1;19(5):654-60.
AbstractLysine acetylation is a reversible post-translational modification (PTM) of cellular proteins and represents an important regulatory switch in signal transduction. Lysine acetylation, in combination with other PTMs, directs the outcomes as well as the activation levels of important signal transduction pathways such as the nuclear factor (NF)-κB pathway. Small molecule modulators of the 'writers' (HATs) and 'erasers' (HDACs) can regulate the NF-κB pathway in a specific manner. This review focuses on the effects of frequently used HAT and HDAC inhibitors on the NF-κB signal transduction pathway and inflammatory responses, and their potential as novel therapeutics.Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.
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