Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Amino Acid Sequence
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Animals
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Drug Discovery*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Histone Demethylases / antagonists & inhibitors*
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Histone Demethylases / chemistry
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Histone Demethylases / metabolism
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Humans
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Models, Molecular
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Molecular Sequence Data
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Peptides / chemistry
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Peptides / pharmacology
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Small Molecule Libraries / chemistry*
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Small Molecule Libraries / pharmacology*
Substances
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Enzyme Inhibitors
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Peptides
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Small Molecule Libraries
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Histone Demethylases