title: A new horizon for epigenetic medicine?
abstract: Histone lysine demethylases are chromatin modifiers that play important roles in many pathological processes such as inflammation and cancer, making them potentially attractive drug targets. In a recent study, Kruidenier et al. provided proof of concept by identifying chemical matters that inhibit demethylation mediated by the two related histone H3 lysine 27 demethylases, KDM6A and 6B (UTX and JMJD3). The KDM6 inhibitor shows remarkable substrate selectivity and can inhibit transcription of a plethora of pro-inflammatory genes in cell culture by altering H3K27me3 level at some of the KDM6 target genes.
authors.affiliation: Division of Newborn Medicine and Program in Epigenetics, Department of Medicine, Boston Children's Hospital and Department of Cell Biology, Harvard Medical School, Boston MA, 02115, USA.
authors.forename: Shuzhen
authors.initials: S
authors.lastname: Chen
authors.forename: Yang
authors.initials: Y
authors.lastname: Shi
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D057890:Epigenomics; D056466:Histone Demethylases / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D056484:Jumonji Domain-Containing Histone Demethylases / Q000037:antagonists & inhibitors / Q000378:metabolism; D008745:Methylation / Q000187:drug effects; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D013379:Substrate Specificity
chemical_list: D004791:Enzyme Inhibitors; D009687:Nuclear Proteins; D056466:Histone Demethylases; D056484:Jumonji Domain-Containing Histone Demethylases; C523998:KDM6A protein, human; C524220:KDM6B protein, human