Histone lysine demethylases as targets for anticancer therapy.

Abstract

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.

• Authors: Jonas W Højfeldt, Karl Agger, Kristian Helin
• Journal: Nature reviews. Drug discovery (Nat Rev Drug Discov) Vol. 12 Issue 12 Pg. 917-30 (Dec 2013) ISSN: 1474-1784 [Electronic] England
• PMID: 24232376 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Antineoplastic Agents
• Histone Deacetylase Inhibitors
• Histone Demethylases

Topics

• Animals
• Antineoplastic Agents (administration & dosage)
• Drug Delivery Systems (methods)
• Histone Deacetylase Inhibitors (administration & dosage, chemistry)
• Histone Demethylases (antagonists & inhibitors, chemistry, metabolism)
• Humans
• Neoplasms (drug therapy, enzymology)