Epigenetics: A new platform for drug discovery

Epigenetic regulators, through interactions with chromatin — modulate the structure, function and accessibility of the genome, thereby impacting gene expression and, ultimately, determining the production or non-production of proteins. The mis-regulation of genes by epigenetic regulators are the source of many diseases and disorders.

Hundreds of epigenetic regulators have recently been identified, many of which are chromatin-binding or chromatin-modifying enzymes, such as histone lysine methyltransferases and demethylases. An increasing number of these enzymes have been associated with diseases.

Drugs directed against this emerging class of gene-regulating enzymes promise entirely novel approaches to the treatment of human disease through preventing the series of chain reactions that are initiated when the enzymes first interact with the chromatin.

Constellation is developing a pipeline of preclinical drug candidates with the initial focus of modulating epigenetic function, particularly histone modifications, to discover and develop novel drugs for oncology. Constellation’s technology platform is also applicable to other therapeutic areas including autoimmune, inflammatory and neurological diseases.

© 2008 Constellation Pharmaceuticals