Recent advances in class IIa histone deacetylases research

Bioorg Med Chem. 2019 Nov 15;27(22):115087. doi: 10.1016/j.bmc.2019.115087. Epub 2019 Sep 6.

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.

Keywords: Anticancer activity; Histone deacetylases; Immune disorders; Neurodegenerative diseases; Synthesis of HDACi.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Epigenomics / methods*
  • Histone Deacetylases / metabolism*
  • Humans

Substances

  • Histone Deacetylases