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The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors.

ABSTRACT: 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.

SUBMITTER: Cao F

PROVIDER: S-EPMC6017514 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature

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The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors.

Cao Fangyuan F Zwinderman Martijn R H MRH Dekker Frank J FJ

Molecules (Basel, Switzerland) 20180302 3

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 ...[more]

PMID: 29498635

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