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. Author manuscript; available in PMC: 2011 Dec 2.
Published in final edited form as: Cancer Cell. 2011 Jan 18;19(1):17–30. doi: 10.1016/j.ccr.2010.12.014

Figure 1. 2-HG Is a Competitive Inhibitor of α-KG for Histone Demethylases.

Figure 1

(A) 2-HG inhibits Caenorhabditis elegans KDM7A demethylase activity. CeKDM7A activities toward H3K9me2 and H3K27me2 peptides were assayed in the presence of increasing concentrations of either D-2-HG or L-2-HG as indicated. The demethylated products were analyzed by mass spectrometry (left) and mean activity values of duplicated assays, represented by percentage of remaining methylated peptides (right), are shown. Error bars represent ± standard deviation (SD) for triplicate experiments.

(B) α-KG rescues 2-HG inhibition of CeKDM7A demethylase activity. Error bars represent ± SD for triplicate experiments.

(C) 2-HG inhibits human JHDM1A/KDM2A demethylase activity. Purified recombinant JHDM1A demethylase activity was assayed in the presence of various concentrations of D-2-HG and L-2-HG as indicated.

(D) α-KG reverses the inhibitory effect of D-2-HG on JHDM1A. JHDM1A activity was assayed in the presence of 50 mM D-2-HG and various concentrations of α-KG.

See also Figure S1.