Evaluation of triazolamers as active site inhibitors of HIV-1 protease

Proteases typically recognize their peptide substrates in extended conformations. General approaches for designing protease inhibitors often consist of peptidomimetics that feature this conformation. Herein we discuss a combination of computational and experimental studies to evaluate the potential of triazole-linked β-strand mimetics as inhibitors of HIV-1 protease activity.

Graphical abstractDesign of nonpeptidic β-strand mimetics as protease inhibitors is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide