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. 2017 Oct 2;61(9):3755–3778. doi: 10.1021/acs.jmedchem.7b00574

Figure 2.

Figure 2

Representative examples of competitive, allosteric, and stabilizing PPI ligands (X-ray structure (above), chemical structure (below)). (A) p53/hDM2 inhibitor RG7112 (PDB ID: 4IPF).43 (B) BH3/Bcl-2 inhibitor ABT-199 (PDB ID: 4MAN).31 (C) Fragment of BRD4/Histone inhibitor I-BET762 (PDB ID: 4C66).32 (D) HIF-2 PAS domain allosteric modulator (PDB ID: 4GHI).35 (E) FKBP12/Rapamycin/FRAP stabilizer complex (PDB ID: 1FAP).40 (F) Transthyretin stabilizer (PDB ID: 2FLM).42