Developing diazirine-based chemical probes to identify histone modification 'readers' and 'erasers'.

Developing diazirine-based chemical probes to identify histone modification ‘readers’ and ‘erasers’† †Electronic supplementary information (ESI) available: experimental methods and figures. See DOI: 10.1039/c4sc02328e Click here for additional data file.

Acetylation- and Methylation-Related Epigenetic Proteins in the Context of Their Targets

The nucleosome surface is covered with multiple modifications that are perpetuated by eight different classes of enzymes. These enzymes modify specific target sites both on DNA and histone proteins, and these modifications have been well identified and termed "epigenetics". These modifications play critical roles, either by affecting non-histone protein recruitment to chromatin or by disturbing...

Bromodomain inhibitors and cancer therapy: From structures to applications

Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes that are "writers," "erasers," or "readers" of histone modification marks are common. Bromodomains are "readers" that bind acetylated lysines in histone tails. Their most important function is the regulation of gene transcription by the recruitment of different molecular partners. Moreover, proteins contain...

EZ Switch From EZH2 to EZH1

An important area of research is the functional significance of posttranslational modifications of histone proteins. The modification of histones is maintained by a balance of enzymes which place specific modifications (writers), factors which read modifications (readers), and enzymes which remove modifications (erasers). Histone methylation is regulated by histone methyltransferases (writers) ...

Seeing beyond the double helix.

Epigenetics, or heritable changes not encoded in the DNA sequence, is a phenomenon important for an overall increase in the complexity of the genome without changes in gene sequence. Our complete genome is contained in each of our cells. Corneal cells are different than nerve cells due to a usage pattern of the genome that is maintained in a cellular memory of active or repressed genes. These “...