Recent Progress in Histone Demethylase Inhibitors

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) a...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2016-02, Vol.59 (4), p.1308-1329
Main Authors: McAllister, Tom E, England, Katherine S, Hopkinson, Richard J, Brennan, Paul E, Kawamura, Akane, Schofield, Christopher J
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Animals
Drug Discovery
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Histone Demethylases - antagonists & inhibitors
Histone Demethylases - chemistry
Histone Demethylases - metabolism
Humans
Models, Molecular
Molecular Sequence Data
Peptides - chemistry
Peptides - pharmacology
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.5b01758