Discovery of new epigenetic drugs among FDA-approved drug libraries
- NJ Raynal, JT Lee, +7 authors W Chung
- In Proceedings: AACR Annual Meeting
L ike stem cell research, epigenetics has been promising radical new therapies, aimed at modifying the expression of target genes for a wide range of diseases. New drugs have been slow to materialize, however, largely because epigenetic mechanisms and their role in gene expression are more complex than originally thought. Nonetheless, clinically approved drugs that target epigenetic mechanisms have become available, and over the few past years, the field has entered a new era that some are calling the second generation of epigenetic drug discovery. This new era is characterized by a more coherent framework for epigenetic drug discovery that goes beyond chasing individual targets as they emerge. The main focus of epigenetic drug discovery efforts has been on cancer, largely because Andrew Feinberg and Ber Vogelstein found altered DNA methylation in cancer in 1983. However, the detailed pathways involved have proved elusive and it has not been easy to separate cause from effect. Meanwhile though, substantial progress has been made understanding and cataloguing the fundamental mechanisms of epigenetic modification of chromatin. These include DNA methylation and histone acetylation, both of which play a key role in gene expression and are implicated in cancer and other conditions.