Immunosilencing peptides by stereochemical inversion and sequence reversal: retro-D-peptides.

ABSTRACT: Peptides are experiencing a new era in medical research, finding applications ranging from therapeutics to vaccines. In spite of the promising properties of peptide pharmaceuticals, their development continues to be hindered by three weaknesses intrinsic to their structure, namely protease sensitivity, clearance through the kidneys, and immune system activation. Here we report on two retro-D-peptides (H₂N-hrpyiah-CONH₂ and H₂N-pwvpswmpprht-CONH₂), which are protease-resistant and retain the original BBB shuttle activity of the parent peptide but are much less immunogenic than the parent peptide. Hence, we envisage that retro-D-peptides, which display a similar topological arrangement as their parent peptides, will expand drug design and help to o

SUBMITTER: Arranz-Gibert P 

PROVIDER: S-EPMC5915530 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature