Figure 5: CP2 derivatives stabilize KDM4A and alter histone methylation status in cells. | Nature Communications

Figure 5: CP2 derivatives stabilize KDM4A and alter histone methylation status in cells.

From: Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

Figure 5

(a) Sequences of peptides with modifications on CP2 (CP2.1, CP2.2 and CP2.3) used for cellular assays. (b,c) KDM4A stability is enhanced for CP2-treated cells in CETSA. (b) CETSA melting curves for Flag-KDM4A in U2OS cells with and without CP2(T13Z) treatment (0.5 μM). The actin Tm was 55 °C for treated and untreated cells. (c) Isothermal dose–response titration CETSAs of dosed U2OS cells at 55 °C demonstrate that both CP2 and CP2.3 stabilize KDM4A in a dose-dependent manner. Average±s.e.m. are shown (n>3, biological). Representative western blotting figures are shown.

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