Højfeldt, Jonas W4; Agger, Karl4; Helin, Kristian4
1 Helin Group, BRIC Research Groups, BRIC, Københavns Universitet2 Administration, BRIC Administration, BRIC, Københavns Universitet3 The Danish Stem Cell Center, Faculty of Health and Medical Sciences, Københavns Universitet4 Helin Group, BRIC Research Groups, BRIC, Københavns Universitet
It has recently been demonstrated that the genes controlling the epigenetic programmes that are required for maintaining chromatin structure and cell identity include genes that drive human cancer. This observation has led to an increased awareness of chromatin-associated proteins as potentially interesting drug targets. The successful introduction of DNA methylation and histone deacetylase (HDAC) inhibitors for the treatment of specific subtypes of cancer has paved the way for the use of epigenetic therapy. Here, we highlight key biological findings demonstrating the roles of members of the histone lysine demethylase class of enzymes in the development of cancers, discuss the potential and challenges of therapeutically targeting them, and highlight emerging small-molecule inhibitors of these enzymes.
Journal review article
Nature Reviews. Drug Discovery, 2013, Vol 12, Issue 12, p. 917-30