Extended Data Fig. 1: Development of YEATS2 YEATS inhibitors by targeting π-π-π stacking. | Nature Chemical Biology

Extended Data Fig. 1: Development of YEATS2 YEATS inhibitors by targeting π-π-π stacking.

From: Complex-specific inhibitors for interrogating ATAC histone acetyltransferase complex

Extended Data Fig. 1: Development of YEATS2 YEATS inhibitors by targeting π-π-π stacking.

a, The complex structure of YEATS2 YEATS-H3K27bz (PDB ID:6LSD). b, Chemical structure of photoaffinity probe Photo-H3K27bz. c, Schematic diagram illustrating the competitive photo-cross-linking assay for determination of inhibitory effects of developed oligopeptides against YEATS domains. d, Three-spot competitive photo-cross-linking assay to screen decapeptides with different modifications at H3K27. e, Histogram showing the inhibitory effects of decapeptides. The relative fluorescence intensity data were quantified from gels shown in d. f, g, ITC measurement for the binding affinities of YEATS2 YEATS toward H3K27cr (f) and H3K27bz (g). h, In-gel fluorescent signal to show the inhibitory effects of LS-08 against AF9, ENL, and GAS41.

Source Data

Back to article page