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. Author manuscript; available in PMC: 2015 Sep 18.
Published in final edited form as: Chem Biol. 2014 Sep 18;21(9):1102–1114. doi: 10.1016/j.chembiol.2014.09.001

Figure 5.

Figure 5

Preclinical examples of inhibitors of PPI with secondary epitopes. A) Crystal structure of menin (white surface) bound to MIV-6R (green sticks, PDB: 4OG8) with MLL peptide overlaid (magenta cartoon, PDB: 3U85). Structures of MLL inhibitors MIV-6R and MIV 2-2. B) Crystal structures of PDK-1, showing the PIF-tide binding site bound with Tethered activator (JS30, green sticks, PDB: 3OTU) or inhibitor (1F8, magenta sticks, 3ORX). JS30 pushes the C-helix into a catalytically competent conformation. Chemical structure of noncovalent PIF-tide inhibitor PS210. C) Structure of OHM1, which binds to CBP at the HIF1α peptide-binding site.