title: Advances and challenges in understanding histone demethylase biology.
abstract: Within the last decade we have witnessed significant progress in the field of chromatin methylation, ranging from the discovery that chromatin methylation is reversible, to the identification of two classes of oxidative chromatin demethylases. Multiple genetic and cellular studies emphasize the role of members of the amine oxidase and 2-oxoglutarate oxygenase enzyme families involved in methyl-lysine in physiology and disease. Advances in understanding of the underlying biochemistry have resulted in development of first series of clinical inhibitors and tool compounds which continue to resolve and help understand the complex relationships between chromatin modification, control of gene expression and metabolic states.
authors.affiliation: Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, UK.
authors.forename: Radoslaw P
authors.initials: RP
authors.lastname: Nowak
authors.affiliation: Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Target Discovery Institute, University of Oxford, OX3 7FZ, UK.
authors.forename: Anthony
authors.initials: A
authors.lastname: Tumber
authors.affiliation: Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, UK; Department of Chemistry, University of Oxford, OX1 3TA, UK.
authors.forename: Catrine
authors.initials: C
authors.lastname: Johansson
authors.affiliation: Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, UK.
authors.forename: Ka Hing
authors.initials: KH
authors.lastname: Che
authors.affiliation: Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Target Discovery Institute, University of Oxford, OX3 7FZ, UK.
authors.forename: Paul
authors.initials: P
authors.lastname: Brennan
authors.affiliation: Pfizer Worldwide Medicinal Chemistry, 610 Main Street, Cambridge, MA 02139, USA.
authors.forename: Dafydd
authors.initials: D
authors.lastname: Owen
authors.affiliation: Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, UK. Electronic address: udo.oppermann@sgc.ox.ac.uk.
authors.forename: Udo
authors.initials: U
authors.lastname: Oppermann
mesh_terms: D002384:Catalysis; D002986:Clinical Trials as Topic; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D044127:Epigenesis, Genetic; D023281:Genomics; D056466:Histone Demethylases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D006657:Histones / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008239:Lysine / Q000378:metabolism; D008745:Methylation
chemical_list: D004791:Enzyme Inhibitors; D006657:Histones; D056466:Histone Demethylases; D008239:Lysine