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Expanding the Druggable Space of the LSD1/CoREST Epigenetic Target: New Potential Binding Regions for Drug-Like Molecules, Peptides, Protein Partners, and Chromatin

Figure 8

Potential small-molecule and peptide LSD1/CoREST druggable sites.

The five most favorable druggable regions thus far unexplored are highlighted using colored spheres and named based on their location: SANT2/Tower interface (green, A), AOD/Tower interface (red, B), SWIRM/AOD interface (blue, C), Peptide binding region (yellow, D), and small AOD pocket (grey, E). LSD1 (orange), CoREST (cyan), and the H3-histone N-terminal tail (purple) are shown as cartoons. Table 1 summarizes the residues in each identified druggable region. See also Figure S2 for a description of the Select-residues criterion used for analysis.

Figure 8