Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation.

Drug Discov Today

Department of Pharmaceutical Gene Modulation, Groningen Research Institute of Pharmacy, University of Groningen, Antonius Deusinglaan, The Netherlands.

Published: June 2011

Post-translational modifications of proteins, such as acetylation, are important regulatory events in eukaryotic cells. Reversible acetylations of histones and non-histone proteins regulate gene expression and protein activity. Acetylation levels of proteins are regulated by a dynamic equilibrium between acetylation by (histone) acetyltransferases and deacetylation by (histone) deacetylases. Alterations in this equilibrium can result in pathological states. Inflammation is a physiological response that, under certain conditions, turns into a disease. This review focuses on the crucial regulatory roles of protein acetylation in NF-κB-mediated inflammation and the potential applications of small-molecule inhibitors of acetylation for the treatment of inflammatory diseases.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5218544PMC
http://dx.doi.org/10.1016/j.drudis.2011.03.009DOI Listing

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