pp 1-30 | Cite as

Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors

  • Daniela TrisciuoglioEmail author
  • Dante RotiliEmail author
Part of the Topics in Medicinal Chemistry book series


The acetylation of lysine residues of histone and nonhistone proteins is a post-translational modification catalysed by the so-called histone acetyltransferases (HATs) that plays a crucial role in several biological settings. The deregulation of this enzymatic activity is implicated in many disease conditions such as cancer and inflammatory and neurological disorders. Despite many histone acetyltransferase inhibitors (HATi) have been identified so far, there is still the need for new, metabolically stable, more potent and selective HATi as potential therapeutic agents and/or as chemical tools for studying HAT biology. In the present chapter, the main features of HAT enzymes and related diseases have been summarized, with a particular focus on HATi, analysing their structure-activity relationships, mechanisms of action and potential therapeutic applications.


Cancer Chemical probes Epigenetics Histone acetyltransferase inhibitors Structure- and ligand-based drug discovery 



Acute lymphoid leukaemia


Acute myeloid leukaemia




CREB-binding protein


Cutaneous squamous cell carcinoma




General control nonderepressible 5


Gcn5-related N-acetyltransferase


Histone acetyltransferase inhibitors


Histone acetyltransferases


Histone deacetylases


Long chain alkylidene malonates


Loss of heterozygosity


Male-specific lethal


Moz, Ybf2/Sas3, Sas2, Tip60


Nuclear receptor coactivator


Non-small-cell lung cancer


Non-specific lethal


p300/CBP-associated factor


Steroid receptor coactivator-1


Steroid receptor coactivator-3/activated in breast cancer-1


TATA box binding protein (TBP)-associated factor


Transcriptional intermediary factor-2


Thyroid hormone receptor activator molecule-1


α-Tubulin acetyltransferase 1


Compliance with Ethical Standards

Conflict of Interest: The authors declare no conflict of interest.

Ethical Approval: This article does not contain any studies with human participants or animals performed by any of the authors.


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Copyright information

© Springer Nature Switzerland AG  2019

Authors and Affiliations

  1. 1.Institute of Molecular Biology and Pathology, National Research CouncilRomeItaly
  2. 2.Preclinical Models and New Therapeutic Agents UnitIRCCS-Regina Elena National Cancer InstituteRomeItaly
  3. 3.Department of Chemistry and Technologies of DrugsSapienza University of RomeRomeItaly

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