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Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.

Abstract:

Ferrous ion and 2-oxoglutarate (2OG) oxygenases catalyze the demethylation of N(epsilon)-methylated lysine residues in histones. Here we report studies on the inhibition of the JMJD2 subfamily of histone demethylases, employing binding analyses by nondenaturing mass spectrometry (MS), dynamic combinatorial chemistry coupled to MS, turnover assays, and crystallography. The results of initial binding and inhibition assays directed the production and analysis of a set of N-oxalyl-d-tyrosine deri...

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Authors


Rose, Nathan R More by this author
Woon, Esther C Y More by this author
Kingham, Guy L More by this author
King, Oliver N F More by this author
Mecinović, Jasmin More by this author
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Journal:
Journal of Medicinal Chemistry
Volume:
53
Issue:
4
Pages:
1810-1818
Publication date:
2010
ISSN:
1520-4804
URN:
uuid:fb6ea5e3-b920-4a8f-9659-f88a8a31c70f
Local pid:
SGC:20088513

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