This hot review from Philip Jones, MD Anderson Cancer Center, Texas, examines our understanding of the structure and function of epigenetic enzymes, including lysine and arginine methyltransferases and demethylases, histone acetyl transferases and histone deacetylases, and the chemical probes and tools available to increase our understanding.
It focuses on the development of a second generation of epigenetic agents able to manipulate histone modifications responsible for aberrant epigenetic gene transcription associated with disease states.
Areas covered:
- Class I and II HDAC inhibitors
- HDAC 1-4, 6, 8 selective inhibitors
- Class III HDAC inhibitors
- Histone acetyl transferase inhibitors
- Histone methyltransferase inhibitors
- Lysine and arginine methyltransferase inhibitors
- Histone demethylase inhibitors
- Lysine specific demethylase 1 inhibitors
- JmJ demethylase inhibitors
Development of second generation epigenetic agents
Philip Jones
DOI: 10.1039/C1MD00199J
This article is part of our forthcoming themed issue on Epigenetics – check back soon for more hot articles in this issue!
