Inhibitors of histone demethylases

Brian Lohse; Jesper L Kristensen; Line H Kristensen; Karl Agger; Kristian Helin; Michael Gajhede; Rasmus P Clausen

doi:10.1016/j.bmc.2011.01.046

Inhibitors of histone demethylases

Bioorg Med Chem. 2011 Jun 15;19(12):3625-36. doi: 10.1016/j.bmc.2011.01.046. Epub 2011 Feb 1.

Authors

Brian Lohse¹, Jesper L Kristensen, Line H Kristensen, Karl Agger, Kristian Helin, Michael Gajhede, Rasmus P Clausen

Affiliation

¹ Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, 2 Universitetsparken, DK-2100 Copenhagen, Denmark.

PMID: 21596573
DOI: 10.1016/j.bmc.2011.01.046

Abstract

Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Binding Sites / drug effects
Enzyme Activation / drug effects
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Histone Demethylases / antagonists & inhibitors*
Humans
Methylation / drug effects
Models, Molecular
Molecular Structure
Substrate Specificity

Substances

Enzyme Inhibitors
Histone Demethylases