Targeting Class I Histone Deacetylases in a “Complex” Environment

Christopher J. Millard, Peter J. Watson, Louise Fairall, John W.R. Schwabe, Trends in Pharmacological Sciences, Available online 28 January 2017, ISSN 0165-6147, doi:10.1016/j.tips.2016.12.006.

Histone deacetylase (HDAC) inhibitors are proven anticancer therapeutics and have potential in the treatment of many other diseases including HIV infection, Alzheimer’s disease, and Friedreich’s ataxia. A problem with the currently available HDAC inhibitors is that they have limited specificity and target multiple deacetylases. Due to their nonselective nature, many patients experience significant side effects.
The focus within the field is turning to the development of isoform-selective HDAC inhibitors to reduce off-target effects experienced by patients.

Targeting Class I Histone Deacetylases in a “Complex” Environment