Abstract
As a class, epigenetic enzymes have been identified as clear targets for cancer therapeutics based on their broad hyperactivity in solid and hematological malignancies. The search for effective inhibitors of histone writers and of histone erasers has been a focus of drug discovery efforts both in academic and pharmaceutical laboratories and has led to the identification of some promising leads. This review focuses on the discovery strategies and preclinical evaluation studies of a subset of the more advanced compounds that target histone writers or histone erasers. The specificity and anticancer potential of these small molecules is discussed within the context of their development pipeline.
Acknowledgements
The authors apologize to all their colleagues whose important work could not be directly cited.
Financial & competing interests disclosure
This work was partly funded by the NIH (R01 CA125269 to E.D.M.; R21AI116222 to I.D./E.D.M), by the Friends of the Cancer Center, by The Welch Foundation (grant I-1878 to E.D.M.) and by CPRIT (RP120717). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.