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Novel cyclic peptides facilitating transcellular blood-brain barrier transport of macromolecules in vitro and in vivo

J Control Release. 2020-03-01; 
Shunsuke Yamaguchi, Shingo Ito, Takeshi Masuda, Pierre-Olivier Couraud, Sumio Ohtsuki
Products/Services Used Details Operation
Peptide Synthesis … spacer in M13 phage. The cyclic peptide AC-SLSHSPQ-CGGGS (cyclic SLS derivative), cyclizing between two cysteines by a disulfide bond, was purchased from GenScript (Tokyo, Japan). Fluorescent cyclic SLS derivative … Get A Quote

摘要

Brain delivery of nanoparticles and macromolecular drugs depends on blood-brain barrier (BBB)-permeable carriers. In this study, we searched for cyclic heptapeptides facilitating BBB permeation of M13 phages by phage library screening using a transcellular permeability assay with hCMEC/D3 cell monolayers, a human BBB model. The M13 phage, which is larger than macromolecular drugs and nanoparticles, served as a model macromolecule. The screen identified cyclic heptapeptide SLSHSPQ (SLS) as a human BBB-permeable peptide. The SLS-displaying phage (SLS-phage) exhibited improved permeation across the cell monolayer of monkey and rat BBB co-culture models. The SLS-phage internalized into hCMEC/D3 cells via macropinoc... More

关键词

Brain delivery, Cyclic peptide, Macromolecule, Phage display technology
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