The Clinically Used Iron Chelator Deferasirox Is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases.
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
Journal
ACS chemical biology
ISSN: 1554-8937
Titre abrégé: ACS Chem Biol
Pays: United States
ID NLM: 101282906
Informations de publication
Date de publication:
16 08 2019
16 08 2019
Historique:
pubmed:
10
7
2019
medline:
4
1
2020
entrez:
10
7
2019
Statut:
ppublish
Résumé
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 potently inhibit JMJD2A (KDM4A)
Identifiants
pubmed: 31287655
doi: 10.1021/acschembio.9b00289
doi:
Substances chimiques
Enzyme Inhibitors
0
Histones
0
Iron Chelating Agents
0
Jumonji Domain-Containing Histone Demethylases
EC 1.14.11.-
KDM4A protein, human
EC 1.5.-
Deferasirox
V8G4MOF2V9
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1737-1750Subventions
Organisme : British Heart Foundation
ID : PG/12/33/29546
Pays : United Kingdom
Organisme : British Heart Foundation
ID : RE/08/004/23915
Pays : United Kingdom
Organisme : Cancer Research UK
ID : C8717/A18245
Pays : United Kingdom