Histone acetyltransferase inhibitors and preclinical studies

Expert Opin Ther Pat. 2009 Jun;19(6):761-74. doi: 10.1517/13543770902895727.


Background: Drugs able to regulate the histone modifier enzymes are very promising tools for the treatment of several diseases, such as cancer. Histone acetyltransferase (HAT) inhibitors are compounds able to inhibit the catalytic activity of HATs reported to be active in cancer, or in several other diseases, such as Alzheimer (AD), diabetes and hyperlipidaemia.

Objectives: Here we review the status and the rationale for the use of HAT inhibitors in the treatment of various diseases.

Methods: Patents have been found on the espacenet database; the clinical trials have been reported as in the clinicaltrial.gov website.

Results and conclusion: Despite the fact that other drugs able to regulate the histone modifier enzymes (such as histone deacetylase inhibitors) have been already approved for the treatment of cancer, HAT inhibitors seem promising for the treatment of human diseases such as AD and diabetes, although side effects and toxicity need to be investigated.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Clinical Trials as Topic
  • Curcumin / pharmacology
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / pharmacology*
  • Histone Acetyltransferases / antagonists & inhibitors*
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / physiopathology
  • Patents as Topic


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Histone Acetyltransferases
  • Curcumin