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Issue 2, 2012
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Inhibition of bromodomain-mediated proteinprotein interactions as a novel therapeutic strategy

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Abstract

A multitude of epigenetic regulatory mechanisms is reflected in the dynamic nature of chromatin during different development stages as well as pathological states of human organisms. Apart from enzymatic processes, the recognition of histone modifications by reader protein modules contributes to the equilibrium between transcriptionally active and silent chromatin. Bromodomains are involved in the recognition of acetylated lysine containing substrates and in the downstream signalling of histone acetylation. In part, this is mediated by the regulation of further acetylation reactions. Development of small molecules as epigenetic tools able to block proteinprotein interactions provided by bromodomains is a new emerging focus of epigenetic research, which also holds great potential for novel therapeutical approaches. This review is dealing with fundamentals of bromodomain structural biology, their inhibitors, and the relevance of these phenomena to molecular biology and drug discovery.

Graphical abstract: Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy

  • This article is part of the themed collection: Epigenetics
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Publication details

The article was received on 04 Aug 2011, accepted on 28 Sep 2011 and first published on 21 Oct 2011


Article type: Review Article
DOI: 10.1039/C1MD00201E
Citation: Med. Chem. Commun., 2012,3, 123-134
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    Inhibition of bromodomain-mediated proteinprotein interactions as a novel therapeutic strategy

    S. D. Furdas, L. Carlino, W. Sippl and M. Jung, Med. Chem. Commun., 2012, 3, 123
    DOI: 10.1039/C1MD00201E

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