Future strategies in epigenetic drug discovery

Download Type: Adobe PDF

Most current research aimed at the discovery of epigenetic therapies adheres to the paradigm of target based drug discovery, focusing on the modulation of single enzymes involved in DNA methylation and histone modifications. The recent discovery of promising small molecule inhibitors for a class of nonenzymatic chromatin regulators, the BET bromodomains, suggests that future drug discovery for epigenetic therapy will involve the modulation of protein–protein interactions and multi-protein complexes.

In this review, Gerard Drewes discusses novel experimental strategies to the discovery of epigenetic drug targets based on assays which more closely reflect physiological complexity. The author outlines different approaches towards the unbiased discovery of small molecule probes for targets that are relevant in the modulation of disease-relevant cellular and epigenetic processes. He also discusses the recent progress in the application of chemical probes in drug discovery utilizing native cellular proteins and protein complexes.

Share this download

More services