There is currently considerable interest in developing an understanding of the roles of epigenetic processes in the development and progression of disease and therefore, in elucidating the potential for modulation of these processes to provide therapeutic benefit. Small molecule inhibitors of epigenetic proteins such as the 'writers', 'erasers' and 'readers' of histone post-translational modifications provide avenues for exploring how modulation of the activities of such proteins affects disease processes. Many of the Jumonji (Jmj) class of proteins have been shown to be members of the histone lysine demethylase class of epigenetic 'erasers'. In this presentation we will report on our efforts towards the discovery of inhibitors of the H3K27 and H3K9 demethylases, JmjD3 and the JmjD2 family respectively, that have demonstrated cellular activity and therefore have potential utility as tool compounds to probe the role of these enzymes in disease.

Novel cell active inhibitors of histone lysine demethylases (KDMs): Progress and challenges in the discovery of tool inhibitors of JumonjiD2 (JmjD2) and JumonjiD3 (JmjD3)

246th National Meeting (2013)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.