Epigenetic small molecule modulators of histone and DNA methylation
Highlights•Histone and DNA methylation are associated with many diseases, esp.
cancer.•Inhibitors of DNA methyltransferases are approved leukemia drugs.•Inhibitors of
lysine methyltransferases and demethylases are in clinical trials.•Inhibitors of arginine
methyltransferases are available as chemical probes.•Methyl lysine binding proteins
(readers) are emerging targets with great potential.DNA and histone methylation belong to
the key regulatory components in the epigenetic machinery, and dysregulations of these …
cancer.•Inhibitors of DNA methyltransferases are approved leukemia drugs.•Inhibitors of
lysine methyltransferases and demethylases are in clinical trials.•Inhibitors of arginine
methyltransferases are available as chemical probes.•Methyl lysine binding proteins
(readers) are emerging targets with great potential.DNA and histone methylation belong to
the key regulatory components in the epigenetic machinery, and dysregulations of these …
Highlights
- Histone and DNA methylation are associated with many diseases, esp. cancer.
- Inhibitors of DNA methyltransferases are approved leukemia drugs.
- Inhibitors of lysine methyltransferases and demethylases are in clinical trials.
- Inhibitors of arginine methyltransferases are available as chemical probes.
- Methyl lysine binding proteins (readers) are emerging targets with great potential.
DNA and histone methylation belong to the key regulatory components in the epigenetic machinery, and dysregulations of these processes have been associated with various human diseases. Small molecule modulators of these epigenetic targets are highly valuable both as chemical probes to study the biological roles of the target proteins, and as potential therapeutics. Indeed, recent years have seen the discovery of chemical modulators of several epigenetic targets, some of which are already marketed drugs or undergoing clinical trials. In this review, we will focus on small molecule modulators of DNA and histone methylation.
Elsevier
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