title: Histone methylases as novel drug targets: developing inhibitors of EZH2.
abstract: Post-translational modifications of histones (so-called epigenetic modifications) play a major role in transcriptional control and normal development, and are tightly regulated. Disruption of their control is a frequent event in disease. In particular, the methylation of lysine 27 on histone H3 (H3K27), induced by the methylase EZH2, emerges as a key control of gene expression and a major regulator of cell physiology. The identification of driver mutations in EZH2 has already led to new prognostic and therapeutic advances, and new classes of potent and specific inhibitors for EZH2 show promising results in preclinical trials. This review examines the roles of histone lysine methylases and demethylases in cells and focuses on the recent knowledge and developments about EZH2.
authors.affiliation: Normandie University, France.
authors.forename: Catherine
authors.initials: C
authors.lastname: Baugé
authors.forename: Céline
authors.initials: C
authors.lastname: Bazille
authors.forename: Nicolas
authors.initials: N
authors.lastname: Girard
authors.forename: Eva
authors.initials: E
authors.lastname: Lhuissier
authors.forename: Karim
authors.initials: K
authors.lastname: Boumediene
mesh_terms: D065150:Cellular Reprogramming; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism; D057890:Epigenomics; D006657:Histones / Q000378:metabolism; D006801:Humans; D063151:Polycomb Repressive Complex 2 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D011110:Polymorphism, Genetic; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D006657:Histones; D054852:Small Molecule Libraries; D063151:Polycomb Repressive Complex 2