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 beta-strand mimetics as inhibitors of HIV-1 protease activity.
Jochim
Andrea L
AL
Department of Chemistry, New York University, 100 Washington Square East, New York, NY 10003, USA.
Miller
Stephen E
SE
Angelo
Nicholas G
NG
Arora
Paramjit S
PS
D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology; D020134:Catalytic Domain; D003198:Computer Simulation; D016333:HIV Protease / Q000737:chemistry* / Q000378:metabolism; D017320:HIV Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D012984:Software; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology
D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D014230:Triazoles; D016333:HIV Protease; C514803:p16 protease, Human immunodeficiency virus 1