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Curr Opin Chem Biol. 2016 Aug;33:151-9. doi: 10.1016/j.cbpa.2016.06.021. Epub 2016 Jun 29.

Advances and challenges in understanding histone demethylase biology.

Author information

1
Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, UK.
2
Structural Genomics Consortium, University of Oxford, Headington OX3 7DQ, UK; Target Discovery Institute, University of Oxford, OX3 7FZ, UK.
3
Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, UK; Department of Chemistry, University of Oxford, OX1 3TA, UK.
4
Pfizer Worldwide Medicinal Chemistry, 610 Main Street, Cambridge, MA 02139, USA.
5
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.

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.

PMID:
27371875
DOI:
10.1016/j.cbpa.2016.06.021
[Indexed for MEDLINE]

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