Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

Epigenetic dysfunction has been widely implicated in several diseases especially cancers
thus highlights the therapeutic potential for chemical interventions in this field. With rapid …

Inhibitors of DNA methyltransferases (DNMTis) or histone deacetylases (HDACis) are
epigenetic drugs which are investigated since decades. Several have been approved and …

Histone methylation reader domains are protein modules that recognize specific histone
methylation marks, such as methylated or unmethylated lysine or arginine residues on …

LSD1 is a histone lysine demethylase proposed as therapeutic target in cancer. Chemical
modifications applied at C2, C4 and/or C7 positions of the quinazoline core of the previously …

Abstract Background Histone posttranslational modifications (PTMs) function to regulate
chromatin structure and function in part through the recruitment of effector proteins that …

The discovery of inhibitors of methyl-and acetyl-binding domains has provided evidence for
the'druggability'of epigenetic effector molecules. The small-molecule probe UNC1215 …

Highlights•Histone and DNA methylation are associated with many diseases, esp.
cancer.•Inhibitors of DNA methyltransferases are approved leukemia drugs.•Inhibitors of …

Modifications of histone tails, including lysine/arginine methylation, provide the basis of a
“chromatin or histone code”. Proteins that contain “reader” domains can bind to these …

Spindlin1 is a histone reader with three Tudor-like domains and its transcriptional co-
activator activity could be attenuated by SPINDOC. The first two Tudors are involved in …