Browsing by Subject "peptidotriazolamers"

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  • Tonali, Nicolo; Hericks, Loreen; Schroeder, David C.; Kracker, Oliver; Krzemieniecki, Radoslaw; Kaffy, Julia; Le Joncour, Vadim; Laakkonen, Pirjo; Marion, Antoine; Ongeri, Sandrine; Dodero, Veronica I.; Sewald, Norbert (2021)
    In peptidotriazolamers every second peptide bond is replaced by a 1H-1,2,3-triazole. Such foldamers are expected to bridge the gap in molecular weight between small-molecule drugs and protein-based drugs. Amyloid beta (A beta) aggregates play an important role in Alzheimer's disease. We studied the impact of amide bond replacements by 1,4-disubstituted 1H-1,2,3-triazoles on the inhibitory activity of the aggregation "hot spots" (KLVFF20)-L-16 and G(39)VVIA(42) in A beta(1-42). We found that peptidotriazolamers act as modulators of the A beta(1-42) oligomerization. Some peptidotriazolamers are able to interfere with the formation of toxic early A beta oligomers, depending on the position of the triazoles, which is also supported by computational studies. Preliminary in vitro results demonstrate that a highly active peptidotriazolamer is also able to cross the blood-brain-barrier.