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Recent Progress in Histone Demethylase Inhibitors

Lookup NU author(s): Dr Tom McAllisterORCiD, Professor Akane Kawamura


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© 2015 American Chemical Society. 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 metadata

Author(s): McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ

Publication type: Review

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2016

Volume: 59

Issue: 4

Pages: 1308-1329

Print publication date: 25/02/2016

Online publication date: 28/12/2015

Acceptance date: 10/11/2015

ISSN (print): 0022-2623

ISSN (electronic): 1520-4804

Publisher: American Chemical Society


DOI: 10.1021/acs.jmedchem.5b01758

PubMed id: 26710088