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There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with small molecules both for the generation of probes for target exploration and for therapeutic purposes. Here we update on previous reviews on the inhibition of the lysine-specific demethylases (LSDs or KDM1s) and JmjC families of N-methyl-lysine demethylases (JmjC KDMs, KDM2-7), focusing on the academic and patent literature from 2014 to date. We also highlight recent biochemical, biological, and structural studies which are relevant to KDM inhibitor development.

Original publication

DOI

10.1021/acs.jmedchem.5b01758

Type

Journal article

Journal

J Med Chem

Publication Date

25/02/2016

Volume

59

Pages

1308 - 1329

Keywords

Amino Acid Sequence, Animals, Drug Discovery, Enzyme Inhibitors, Histone Demethylases, Humans, Models, Molecular, Molecular Sequence Data, Peptides, Small Molecule Libraries