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Brian Lohse, Anders L. Nielsen, Jan B. L. Kristensen, Charlotte Helgstrand, Paul A. C. Cloos, Lars Olsen, Michael Gajhede, Rasmus P. Clausen and Jesper L. Kristensen Targeting Histone Lysine Demethylases by Truncating the Histone 3 Tail to Obtain Selective Substrate-Based Inhibitors Angewandte Chemie International Edition 50

Version of Record online: 25 AUG 2011 | DOI: 10.1002/anie.201101849

Thumbnail image of graphical abstract

How low can you go? The natural substrate for the epigenetic regulators PHF8, JmjD2A, and JmjD2C (lysine demethylases), a peptide consisting of 39 amino acid residues, can be truncated to 14, 8, and 4 amino acids, respectively, while maintaining catalytic activity (see picture). Inhibitors were prepared by attaching small molecules to the truncated substrates. Selective inhibition of JmjD2C over JmjD2A and PHF8 was possible.

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