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The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors

Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, 9713AV Groningen, The Netherlands
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Molecules 2018, 23(3), 551; https://doi.org/10.3390/molecules23030551
Received: 29 January 2018 / Revised: 21 February 2018 / Accepted: 27 February 2018 / Published: 2 March 2018
(This article belongs to the Special Issue Modulators of Histone Acetylation: A Medicinal Chemistry Perspective)
Histone deacetylases (HDACs) are epigenetic drug targets that have gained major scientific attention. Inhibition of these important regulatory enzymes is used to treat cancer, and has the potential to treat a host of other diseases. However, currently marketed HDAC inhibitors lack selectivity for the various HDAC isoenzymes. Several studies have shown that HDAC3, in particular, plays an important role in inflammation and degenerative neurological diseases, but the development of selective HDAC3 inhibitors has been challenging. This review provides an up-to-date overview of selective HDAC3 inhibitors, and aims to support the development of novel HDAC3 inhibitors in the future. View Full-Text
Keywords: histone deacetylase 3 (HDAC3); selective; drug discovery; inhibitor; isoenzyme histone deacetylase 3 (HDAC3); selective; drug discovery; inhibitor; isoenzyme
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MDPI and ACS Style

Cao, F.; Zwinderman, M.R.H.; Dekker, F.J. The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors. Molecules 2018, 23, 551.

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