Stapled Peptides for Intracellular Drug Targets

De Novo Design and Their Antimicrobial Activity of Stapled Amphipathic Helices of Heptapeptides

“…All-hydrocarbon peptide stapling is a powerful cross-linking system that effectively stabilizes the α-helical conformation of a peptide by incorporating an all-hydrocarbon tether formed via ruthenium-mediated ringclosing olefin metathesis. [17][18][19][20][21] For the hydrophobic face, we placed the oct-4-enyl staple between position 2 and 6 ( Figure 1). For the hydrophillic face, a lysine was incorporated at positions 1, 4, and 7 each, which reside on the opposite side of the staple.…”

Regulation of protein–protein interactions using stapled peptides

“…2,3 Proteomimetics, and stapled peptides in particular, are proving useful for targeting PPIs. 4,5 The main focus of this review is the design, synthesis, and application of stapled peptides as molecular probes to disrupt PPIs. …”

In silico study of peptide inhibitors against BACE 1

“…Even though high biodegradability, low bioavailability and low cellular uptake may be some of the limitations of peptide drugs, they can benefit from novel synthetic strategies for enhancing their drug-like properties (Pandey et al 2009;Vlieghe et al 2010). Currently, modifications that a prospective peptide drug candidate can undergo to enhance their efficacy include peptide stapling (Verdine and Hilinski 2012), backbone replacement (Fernández-Llamazares et al 2014), non-natural amino acid incorporation, pseudo peptide bonds, cyclization (Gentilucci et al 2010), conjugation (Gauthier and Klok 2008;Ahrens et al 2012) and so on.…”