Back to article: Inhibitors of glycosomal protein import provide new leads against trypanosomiasis


FIGURE 2: Structure based design of the inhibitors of PEX5-PEX14 interaction. (A) Structure of Trypanosoma PEX14 N-terminal domain bound to PEX5 diaromatic pentapeptide motif. (B) 3D-Pharmacophore model generat-ed on the basis of the structure. Spatial placements of hydrophobic moieties were defined as spheres on protein surface. (C) X-ray crystal structure of inhibitor bound Trypanosoma PEX14. The molecule satisfies pharmacophore model and is able to outcompete PEX5 from PEX14 binding interface.

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