The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors

Fangyuan Cao; Martijn R H Zwinderman; Frank J Dekker

doi:10.3390/molecules23030551

The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors

Fangyuan Cao, Martijn R H Zwinderman, Frank J Dekker

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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.

Original language	English
Article number	551
Number of pages	13
Journal	Molecules
Volume	23
Issue number	3
DOIs	https://doi.org/10.3390/molecules23030551
Publication status	Published - 2-Mar-2018

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Journal Article
Review

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10.3390/molecules23030551Licence: CC BY

The Process and Strategy for Developing SelectiveFinal publisher's version, 2.87 MBLicence: CC BY

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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.",

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N2 - 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.

AB - 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.

KW - Journal Article

KW - Review

U2 - 10.3390/molecules23030551

DO - 10.3390/molecules23030551

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JO - Molecules

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The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors

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