Histone Deacetylases (HDACs): Evolution, Specificity, Role in Transcriptional Complexes, and Pharmacological Actionability

• Published in: Genes Vol. 11; no. 5; p. 556
• Main Authors: Milazzo, Giorgio, Mercatelli, Daniele, Di Muzio, Giulia, Triboli, Luca, De Rosa, Piergiuseppe, Perini, Giovanni, Giorgi, Federico M.
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 15.05.2020; MDPI
• Subjects: antineoplastic agents; Antineoplastic Agents - therapeutic use; Arthropods; Cell cycle; Chelonia mydas; chromatin; Chromatin remodeling; Enzymes; Eukaryotes; Evolutionary conservation; Gene expression; Genomes; HDAC protein; Histone deacetylase; Histone Deacetylase Inhibitors - therapeutic use; Histone Deacetylases - genetics; Histones; Histones - genetics; Humans; Insects; Mammals; moieties; Nematodes; Neoplasms - genetics; Neoplasms - therapy; Organisms; Pathogenesis; Phylogenetics; Proteins; Reptiles & amphibians; Review; Substrate Specificity - genetics; tissues; Transcription; transcription (genetics); Transcription Factors - genetics; Yeast; Zebrafish; gene networks; phylogenesis; epigenomics; histone deacetylases; HDAC inhibitors; cancer; chromatin; HDACi; epigenetics; HDAC
• ISSN: 2073-4425; 2073-4425
• DOI: 10.3390/genes11050556

Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by removing acetyl groups from histones and other protein regulatory factors, with functional consequences on chromatin remodeling and gene expression profiles. We provide here a review on the recent knowledge accrued on the zinc-dependent HDAC protein family across different species, tissues, and human pathologies, specifically focusing on the role of HDAC inhibitors as anti-cancer agents. We will investigate the chemical specificity of different HDACs and discuss their role in the human interactome as members of chromatin-binding and regulatory complexes.