Recent advances in class IIa histone deacetylases research.

Yodita Asfaha, Christian Schrenk, Leandro A Alves Avelar, Alexandra Hamacher, Marc Pflieger, Matthias U Kassack, Thomas Kurz

Journal: Bioorganic & medicinal chemistry 2020;27(22):115087

PMID: 31561937

Full Text on Elsevier Science View on PubMed

Abstract

Epigenetic control plays an important role in gene regulation through chemical modifications of DNA and post-translational modifications of histones. An essential post-translational modification is the histone acetylation/deacetylation-process which is regulated by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The mammalian zinc dependent HDAC family is subdivided into three classes: class I (HDACs 1-3, 8), class II (IIa: HDACs 4, 5, 7, 9; IIb: HDACs 6, 10) and class IV (HDAC 11). In this review, recent studies on the biological role and regulation of class IIa HDACs as well as their contribution in neurodegenerative diseases, immune disorders and cancer will be presented. Furthermore, the development, synthesis, and future perspectives of selective class IIa inhibitors will be highlighted.

Address: Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225 Düsseldorf, Germany.; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225 Düsseldorf, Germany. Electronic address: [email protected].; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225 Düsseldorf, Germany. Electronic address: [email protected].

DOI: 10.1016/j.bmc.2019.115087

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MeSH Terms: Epigenomics, Histone Deacetylases, Humans