The Clinically Used Iron Chelator Deferasirox Is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases

• Published in: ACS chemical biology Vol. 14; no. 8; pp. 1737 - 1750
• Main Authors: Roatsch, Martin, Hoffmann, Inga, Abboud, Martine I, Hancock, Rebecca L, Tarhonskaya, Hanna, Hsu, Kuo-Feng, Wilkins, Sarah E, Yeh, Tzu-Lan, Lippl, Kerstin, Serrer, Kerstin, Moneke, Isabelle, Ahrens, Theresa D, Robaa, Dina, Wenzler, Sandra, Barthes, Nicolas P. F, Franz, Henriette, Sippl, Wolfgang, Lassmann, Silke, Diederichs, Sven, Schleicher, Erik, Schofield, Christopher J, Kawamura, Akane, Schüle, Roland, Jung, Manfred
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 16.08.2019
• Subjects: Catalytic Domain - drug effects; Cell Line, Tumor; Deferasirox - pharmacology; Demethylation - drug effects; Enzyme Inhibitors - pharmacology; Epigenesis, Genetic - drug effects; Histones - metabolism; Humans; Iron Chelating Agents - pharmacology; Jumonji Domain-Containing Histone Demethylases - antagonists & inhibitors; Jumonji Domain-Containing Histone Demethylases - chemistry

Fe­(II)- and 2-oxoglutarate (2OG)-dependent JumonjiC domain-containing histone demethylases (JmjC KDMs) are “epigenetic eraser” enzymes involved in the regulation of gene expression and are emerging drug targets in oncology. We screened a set of clinically used iron chelators and report that they po...